Category: 5233-42-1

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

Dichloro-isoproterenol (I) is known to prevent both adrenaline (II)-induced increase of contractile force and activation of phosphorylase in the dog heart in situ. The present study demonstrates that I almost completely abolishes the increase in blood sugar and free fatty acids induced by II, noradrenaline (III), and isoproterenol in the dog. The hyperlactic-acidemic effect of II is partly blocked. I does not block II-induced hyperglycemia in mice. In contrast to I, phenoxybenzamine (IV) does not affect the hyperglycemia or increase in blood lactic acid induced by II in the dog. Ergotamine antagonizes the hyperglycemia but not the increase in lactic acid. IV effectively blocks the vasopressor response to II and III, and ergotamine produces maximal reversal of II. None of these drugs in the doses used antagonized the pos. inotropic effect of adrenergic stimuli. Both I and IV increase blood glucose and lactic acid. High doses of I appear to antagonize the hyperglycemic action of low doses. The hyperglycemia and lactic acid increase produced by IV are antagonized by I. I also produces a marked and sustained increase in free fatty acids even with doses which do not block the action of II. Possible mechanisms of action are discussed.

Effect of adrenergic blocking agents on some metabolic actions of catechol amines. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

As compared with chlorothiazide, the effect of hydrochlorothiazide (I) was 10-fold stronger. Its effect could be increased further by introducing a dichloromethyl group at C-3, or by building a 3rd ring into the compound at this point. The resulting 3,3-pentamethylene-I and 3,3-(3-thiapenta-methylene)-I were 2-4-fold more effective than I. The I derivatives increased Na excretion. As long as a Na excess was present in the organism, the K excretion was not affected. Extirpation of the adrenals did not alter the effect of I if the rats were kept on a physiol. sufficient cortexone and hydrocortisone regimen. Excess cortexone doses >1.5 mg./kg. or >0.1 mg. aldosterone/kg. inhibited the I effect.

Diuretic effect of hydrochlorothiazide derivatives. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

A simple, sensitive, and reproducible ultra-performance liquid chromatog. (UPLC) method for the determination of nine known potential impurities present in Olmesartan medoxomil and Hydrochlorothiazide tablets in fixed dose combination drug product was developed. Chromatog. separation was achieved between impurities at satisfactory level using Acquity UPLC HSS T3, 100 mm length ¡Á 2.1 mm id with 1.8 ¦Ìm particle size column. Gradient elution mode was kept using mobile phase A as 0.1% orthophosphoric acid buffer adjusted the pH 2.5 and acetonitrile as mobile phase B. Flow rate was kept at 0.5 mL min-1 with a monitoring wavelength of 225 nm. The method is fast and uses less consumption of solvents with shorter run time of 9 min. This can enable the separation of all known potential impurities of two active compounds in a rapid, precise, sensitive, cost, and time effective manner. The performance of the method was validated according to the present ICH guidelines for specificity, limit of detection, limit of quantification, linearity, accuracy, precision, solution stability, and robustness. The method is fast and is suitable for high-throughput anal. of the drug facilitating the processing of large-number batch samples.

Method Development and Validation for the Determination of Potential Impurities Present in Olmesartan Medoxomil and Hydrochlorothiazide in Fixed Dose Combination Drug Product by Using Reverse Phase – Ultra-Performance Liquid Chromatography Coupled with Diode-Array Detector. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

A series of 3-substituted 3,4-dihydro-1,2,4-benzothiadiazine 1,1-dioxides was synthesized by condensation of substituted orthanilamides with aldehydes and the compounds tested for their efficacy as diuretic agents. Some side products and unusual reactions which occurred in the application of the general synthetic method were examined The following acetals were prepared by known methods: the diethyl acetals of bromochloroacetaldehyde, iodoacetaldehyde, dibromoacetaldehyde, ¦Á-bromoisovaleraldehyde, ¦Á-bromopropionaldehyde, ¦Á-bromomethylbutyraldehyde, phenylglyoxal, methylthioacetaldehyde, benzylthioacetaldehyde, phenylthioacetaldehyde, phenoxyacetaldehyde, p – chloro-, p-methyl-, and p-methoxyphenylacetaldehydes, and carbethoxyacetaldehyde; the dimethylacetals of ¦Á-bromophenylacetaldehyde and ¦Á-chlorophenylacetaldehyde; and the dipropyl acetal of ¦Á,¦Á-dichloropropionaldehyde. With the exception of p-isopropylphenyl- and 2,4,6-trimethylphenylacetaldehydes, the requisite aldehydes were com. available. The following general methods were used in the condensation of the substituted orthanilamide with various aldehydes. The yields varied from 30 to 90% and optimum conditions were not determined Method A. The substituted orthanilamide (0.01 mole) and 0.2 mole aldehyde component was refluxed 12 hrs. in 25-50 ml. MeCN, the solvent and excess aldehyde evaporated, and the residue crystallized Method B. The orthanilamide and 2 molar equivalents aldehyde (or its acetal) in alc.-HCl were refluxed 1-2 hrs., concentrated, diluted with CHCl3, concentrated, the mixture cooled, the product collected, washed, and recrystallized Method C. The orthanilamide (5 g.), 15-30 ml. acetal, and enough 18% alc.-HCl was heated 30-60 min. at 110-150¡ã, the alc. distilled, the mixture cooled, the solid filtered off, and washed with Et2O. In cases where the product did not crystallize, the excess solvent was removed and the residue triturated with Et2O. Method D. A mixture of the substituted orthanilamide and 1.1 equivalents aldehyde was heated 1 hr. at 200¡ã, cooled, and the crude product recrystallized The following 7-sulfamoyl-dihydrobenzothiadiazine 1,1-dioxides were thus obtained (6-, 5-, 3-substituents, method of preparation, m.p., and recrystallization solvent given): Cl, H, Me, A, 256¡ã, EtOAc-hexane; Cl, Cl, Me, A, 268-9¡ã, EtOAc-hexane; Cl, H, Et, A, 269-70¡ã, tetrahydrofuran-CHCl3; Cl, H, Pr, B, 247¡ã, MeOH-CHCl3; Cl, H, iso-Pr, A, 308-9¡ã, MeCN; Cl, H, Bu, B, 213¡ã, MeOH-CHCl3; CF3, H, Bu, B, 174-5¡ã, EtOAc-CHCl3; Cl, H, iso-Bu, B, 228¡ã, MeOH-CHCl3; Cl, H, tert-Bu, B, 326-7¡ã MeOH; Cl, H, C5H11, B, 207-8¡ã, MeOH-CHCl3; Cl, H, CH2Cl, C, 239-40¡ã, EtOAc-hexane; Cl, H, CH2Br, C, 216-17¡ã EtOAc-hexane; Cl, H, CH2I, C, 214¡ã, EtOAc-hexane; Cl, H, CHBrMe, C, 252-3¡ã, EtOAc-hexane; Cl, H, CHBrPr-iso, C, 180¡ã, EtOAc-hexane; Cl, H, CBrMeEt, C, 188-9¡ã, EtOAc-hexane; Cl, H, CHCl2, B, 280-1¡ã, MeOH-CHCl3; Br, H, CHCl2, B, 264-6¡ã, MeOH-CHCl3; F, H, CHCl2, B, 266¡ã, MeOH-CHCl3; CF3, H, CHCl2, B, 259-60¡ã, MeOH-CHCl3; Cl, H, CHClBr, C, 256¡ã, EtOAc-hexane; Cl, H, CHBr2, C, 247¡ã, EtOAc; Cl, H, CHF2, B, 296-7¡ã, MeOH-CHCl3; Cl, H, CCl2Me, B, 285¡ã, Me2COCHCl3; Cl, H, CMe2CH2OH, B, 250-1¡ã, MeOH; Cl, H, CH2OEt, B, 223¡ã, alc.-CHCl3; Cl, H, CH2COMe, C, 210¡ã, alc.-hexane; Cl, H, glycidyl, A, 246¡ã, MeCN; Cl, H, CH2SMe, B, 216-17¡ã, EtOAc-CHCl3; Cl, H, CH2CO2Et, B, 216-17¡ã, MeOH-CHCl3; Cl, H, CH2NH2, B, 178-80¡ã, Me2CO-pentane; Cl, H, piperidinomethyl, B, 173-5¡ã, EtOAc-hexane; Cl, H, Ph, B, 241-2¡ã, Me2CO-pentane; Cl, H, p-ClC6H4, D, 258-9¡ã, MeOH-CHCl3; Cl, H, o-ClC6H4, D, 272-4¡ã, MeOH-CHCl3; Cl, H, 2,4-(MeO)2C6H3, D, 211-12¡ã, MeOH; Cl, H, 3,4,5-(MeO)3C6H2, B, 244-6¡ã, Me2CO-CHCl3; Cl, H, p-EtO2CC6H4, B, 255-6¡ã, MeOH; Cl, H, p-HO2CC6H4, D, 289-90¡ã, tetrahydrofuran-CHCl3; Cl, H, 2-furyl, B, 190-5¡ã, MeOH-CHCl3; Cl, H, 2-thienyl, D, 211-13¡ã, MeOH-CHCl3; Cl, H, 2-(5-nitrofuryl), B, 239¡ã, MeOH-CHCl3; Cl, H, CH2Ph, C, 267-8¡ã, MeOH; Br, H, CH2Ph, B, 266¡ã, Me2CO-CHCl3; CF3, H, CH2Ph, B, 228¡ã, MeOH-CHCl3; Cl, H, p-MeC6H4CH2, B, 242-4¡ã, MeOH; Cl, H, p-iso-PrC6H4CH2, B, 232-3¡ã, EtOAc-hexane; Cl, H, 2,4,6-Me3C6H2CH2, B, 276-8¡ã, tetrahydrofuran-CHCl3; Cl, H, p-ClC6H4CH2, B, 245-6¡ã, MeOH-Et2O; Cl, H, p-MeOC6H4CH2, B, 239-41¡ã, MeOH; Cl, H, 3,4-(MeO)2C6H3CH2, B, 250-1¡ã, alc.; Cl, H, CHMePh, B, 231-2¡ã, EtOAc-hexane; Cl, H, CH2CH2Ph, B, 230¡ã, MeOH-CHCl3; CF3, H, CH2CH2Ph, B, 234-6¡ã, EtOAc-hexane; Cl, H, (CH2)3Ph, B, 214-15¡ã, MeOH-CHCl3; Cl, H, CH2OPh, B, 257¡ã, Me2CO-CHCl3; Cl, H, CH2SPh, B, 211-13¡ã, MeOH-CHCl3; Cl, H, CH2SCH2Ph, B, 218-19¡ã, MeOH-CHCl3; Cl, H, 3-cyclohexenyl, A, 248-9¡ã, MeOH-CHCl3; Cl, H, Cú·CPh, C, 238-9¡ã, alc.-hexane; Cl, H, 1-(2,5-endo-methylene-3-ethoxycarbonylcyclohexyl), B, 245-7¡ã, MeOH-hexane. HCHO (1.2 g., 36-8%) added to 2.94 g. 5-chloro-2,4-disulfamoylaniline in 5 ml. MeOH, the mixture refluxed 1 hr., evaporated, the residue dissolved in H2O, and cooled gave 2.05 g. 6-chloro-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine, 1,1-dioxide, m. 266.5-7.5¡ã. Essentially the same procedure was used in the preparation of 5,6-dichloro-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 307-9¡ã (H2O), and the 5-methyl-6-chloro analog, m. 302-3¡ã (alc.-H2O). 5-Chloro-2,4-disulfamoylaniline (2.5 g.), 3 g. dichloroacetal, 25 ml. 18% alc.-HCl, and 0.25 ml. H2O refluxed 5 hrs., evaporated, cooled, treated with CHCl3, and refrigerated overnight gave 2 g. 6-chloro-3-dichloromethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. Difluoroacetic acid (17.9 g.) and 31 g. benzotrichloride containing a little ZnCl2 heated to reflux until HCl evolution ceased and distilled gave 15.6 g. difluoro-N,N-dimethylacetamide (I), b12 101-2¡ã. I (3.1 g.) in 150 ml. Et2O treated in 15 min. with Li diethoxyaluminum hydride in 30 ml. Et2O, the mixture stirred overnight at room temperature, a saturated aqueous solution of 5 ml. Na2SO4 then 70 g. anhydrous Na2SO4 added, the mixture filtered, the ether filtrate added to 25 ml. 4% HCl-alc., and treated with 1 g. 5-chloro-2,4-disulfamoylaniline gave 0.83 g. 6-chloro-3-difluoromethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. The crude HCl salt (prepared by method C) in 100 ml. hot dilute AcOH filtered, brought to pH 8, and cooled gave 1.1 g. 6-chloro-3,4-dihydro-3-piperidinomethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 173-5¡ã (decomposition). When recrystallized from Me2CO-pentane, a solvate was obtained containing one mole Me2CO. The crude HCl salt of 3-amino-methyl-3,4-dihydro-6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide in hot H2O cooled, treated with one equivalent aqueous KOH, and cooled gave the free base. 5-Chloro-2,4-disulfamoylaniline (5 g.), 25 ml. chloral, and 5 drops concentrated H2SO4 refluxed 2 hrs., the mixture diluted with CHCl3, and the crude product crystallized gave 2.8 g. 6-chloro-3,4-dihydro-7-sulfamoyl-3-trichloromethyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 301-2¡ã (decomposition) (MeOH-CHCl3). 5-Chloro-2,4-disulfamoylaniline (5 g.), 25 ml. ethoxyacetal, 100 ml. tetrahydrofuran, and 1 ml. 18% alc.-HCl kept 12 hrs. at room temperature gave 0.77 g. 5-chloro-3,4-disulfamoyl-1-(2-ethoxyethylideneamino)benzene, m. 350¡ã (tetrahydrofuran). 5-Chloro-2,4-disulfamoylaniline (2 g.) and 1.98 g. p-CIC6H4CHO heated 0.5 hr. at 230-40¡ã gave 2 products, m. 257-8¡ã and m. 360¡ã, the 1st assigned the structure 6-chloro-3-(p-chlorophenyl)-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide and the 2nd the structure 5-chloro-1-(p-chlorobenzylideneamino)-2,4 -disulfamoylbenzene. 5-Chloro-2,4-disulfamoylaniline (5 g.) and 5.15 g. 3,4,5-trimethoxybenzaldehyde heated 0.5 hr. at 220-5¡ã gave 1.75 g. 5-chloro-2,4-disulfamoyl-1-(3,4,5-trimethoxybenzylideneamino)benzene, m. 300¡ã (MeOH). The same starting material heated 1 hr. with 40 ml. 2% alc.-HCl gave 4.8 g. 6-chloro-3,4-dihydro-7-sulfamoyl-3-(3,4,5-trimethoxyphenyl)-1,2,4-benzothiadiazine 1,1-dioxide, m. 244-6¡ã. Attempted crystallization from MeOH-CHCl3 gave a high yield of starting material. 5-Chloro-2,4-disulfamoylaniline (1 g.) and 0.68 g. o-carboxybenzaldehyde fused 1 hr. at 200-5¡ã gave 0.6 g 5-chloro-1-(2-carboxybenzylideneamino)-2,4-disulfamoylbenzene (II), m. 354¡ã (tetrahydrofuran-CHCl3). The same starting material warmed 1 hr. with 10 ml. 2% alc.-HCl gave 1.35 g. II. 5-Chloro-2,4-disulfamoylaniline (5 g.) heated with 15 ml. BzH gave 7.6 g. crude 7-benzylidenesulfamoyl-6-chloro-3,4-dihydro-3-phenyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 241-2¡ã (Me2CO-pentane). 5-Chloro-2,4-disulfamoylaniline (5 g.), 3.78 g. glycidaldehyde, and 50 ml. 20% alc.-HCl heated 5-10 min., then refluxed 20 min. gave 3.17 g. 6-chloro-3-¦Â-hydroxyethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (III), m. 320-1¡ã (decomposition) (alc.). 6-Chloro-3-epoxyethyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1 – dioxide (0.5 g.) heated 15 min. with 20% alc.-HCl gave 0.42 g. III. 5-Chloro-2,4-disulfamoylaniline (10 g.) and 15 g. dihydroxyacetone in 50 ml. 18% alc.-HCl refluxed 6 hrs., cooled, triturated with Et2O, filtered, and recrystallized gave 12 g. III. 5-Chloro-2,4-disulfamoylaniline (2.8 g.), 1 g. glyceraldehyde, 18 ml. alc., and 12 ml. 30% alc.-HCl refluxed 15 min. gave 1.6 g. III. 5-Chloro-2,4-disulfamoylaniline (4.5 g.), 9 g. phenylglyoxal diethyl acetal, and 70 ml. 8% alc.-HCl heated 2 hrs. gave 2.42 g. 6-chloro-3-(¦Á-hydroxybenzyl) – 7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 282-3¡ã (decomposition). 2,3-Dichloro-4,6-disulfamoylaniline (10 g.) in 800 ml. 95% alc. refluxed overnight with 23 g. 30% aqueous glyoxal gave 2.95 g. 5,6-dichloro-3-hydroxymethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 278-80¡ã (decomposition) (Me2CO). III (5.9 g.) in 250 ml. tetrahydrofuran refluxed 21 hrs. with 5.9 g. NaBH4 gave 1.72 g. 6-chloro-3,4-dihydro-3-¦Â-hydroxyethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide, m. 234¡ã (decomposition). An analogous procedure was used for the preparation of 5,6-dichloro-3,4-dihydro-3-hydroxymethyl-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide. 5-Chloro-2,4-disulfamoylaniline (2 g.), 2.8 g. ¦Á-chlorophenylacetaldehyde dimethyl acetal, 100 ml. alc., 40 ml. 23% alc.-HCl, and 3 drops H2O refluxed 1 hr. gave 6-chloro-3-¦Á-chlorobenzyl-3,4-dihydro-7-sulfamoyl-1,2,4-benzothiadiazine 1,1-dioxide (IV), m. 182-4¡ã (decomposition), after drying in vacuo m. 198-205¡ã (decomposition). 5-Chloro-2,4-disulfamoylaniline (2 g.), 3.4 g. ¦Á-bromophenylacetaldehyde dimethyl acetal, 100 ml. alc., 40 ml. 23% alc.-HCl, and 3 drops H2O treated as above gave 1.4 g. IV. The ultraviolet absorption spectra were given for a number of the above compounds

3-Substituted dihydrobenzothiadiazine 1,1-dioxides as diuretic agents. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

Evidence obtained previously from in vivo experiments indicated that there are some possible relations between the diuretic actions and the physiol. dispositions of several sulfonamide diuretics. In the present investigation, tubular transport of these compounds was studied in slices of the rat kidney by a modification of the method developed by Cross and Taggart for PAH (p-aminohippuric acid) (CA 44, 6037h). Chem. determinations of these compounds were carried out by a modification of Baer, et al. (loc. cit) and S/M ratios (ratios of concentrations of drug in slice vs. medium after incubating at 25¡ã for 2 hrs.) were calculated Both HCT (hydrochlorothiazide) and PAH accumulated to a considerable degree in the renal slices. The S/M ratios of these compounds were 9.3 and 7.2, resp. However, when the incubation was carried out at 37¡ã, the S/M ratios of both drugs decreased appreciably in spite of an increase of QO2. Variations from an optimal pH of 7.8 to 8.0 towards either the acid or alk. side produced a decrease of S/M values for both drugs. Anaerobic conditions inhibited, while addition of acetate stimulated, the accumulation of HCT in the slices. Dinitrophenol (2.5 ¡Á 10-5M) or cyanide (50-100 ¡Á 10-5M) decreased the S/M values of PAH, CT (chlorothiazide), and HCT considerably. Diodrast or penicillin G, when added in concentrations 15 times as high as that of the substrate, also decreased the S/M value of HCT, without affecting the QO2 of the slices. These results suggest that HCT and its analogs may share a common renal transport mechanism with PAH, penicillin G, and Diodrast. In addition, the S/M values of 8 sulfonamide diuretics (including CT and HCT) were compared. It was found that those compounds such as HCT-55 (5-chlorohydrochlorothiazide), HCT, and HFT (hydroflumethiazide) which showed relatively high diuretic activities also exhibited higher S/M values. On the contrary, inactive compounds or compounds with low diuretic activities, such as HCT-18 (3-[3,4-dimethoxy-2-ethoxycarbonylphenyl]hydrochlorothiazide), CT, and DSA (5-chloro-2,4-disulfamylaniline) had lower S/M values. These results would be in favor of the concept that these sulfonamide derivatives exert their diuretic actions in the process of being transported by the renal tubular epithelium. CT-S (benzthiazide) accumulated in the liver slices of the rat to the same extent as in the renal slices, while HCT accumulated preferentially in the kidney slices.

Oral diuretics. IV. The uptake of some sulfonamide diuretics by rat renal slices. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

1. The impurity of diuretic hydrochlorothiazide 04, also be a medical intermediate.
2. It’s mainly used for the detection of drug impurities, the synthesis of hydrochlorothiazide and the screening of medical structural fragments.
3. Presents a weak alkaline,refrigeration.

. Recommended Products is: 5250-72-6 and 22503-72-6.

Chlorothiazide, 6-chloro-7-sulfamoyl-1,2,4-benzothiadiazine 1,l-dioxide, yields a 3,4-dihydro derivative, hypothiazide (I). Taking the diuretic and saluretic activities (in rats) of chlorothiazide as 1, resp. activities of I were 4.1, 10.8; among derivatives, peak activity (16.0, 40.0) was reached with pentamethylene instead of the 2 H atoms in the 3-position. Other activating substitutions were 5-Cl (5.8, 4.0); 3-Me (1.7, 4.0); 3-CCl3 (1.1, 6.2); and ring rupture at 2 to form 1-SO2NH2 and NHCH2OMe groups (3.5, 7.5). Other substitutions, giving activities less than 1, were 6-NH2, 3-H (no activity), 5-Br. After ring rupture the groups SO2NHMe (0.7, 0.9) and SO2NEt2 (0,0) lowered activity. Effective diuretic doses (mg./kg.) were determined for I derivatives in which the 3-CH2 group is replaced: CHEt 0.5; CHCH:CH2 0.2; CHCH:CHMe 1.0; and side rings, 4-methylcyclohexyl 4.0; cyclopentyl 0.2; thiacyclohexyl 0.2; dithiacyclopentyl 0.1; piperidyl 4.0; N-ethylpiperidyl 4.0; I 0.2. The relatively inactive N-ethylpiperidyl derivative had a pronounced hypotensive effect.

Diuretic effects of dihydrochlorothiazide derivatives. Recommended basis is hydrochlorothiazide 20. Products is: https://www.ambeed.com/products/742-20-1.html, 432499-63-3

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem