Tag: M.W=150-200

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

A palladium-catalyzed method for the decarboxylative ortho C-H acylation of N-sulfoximine benzamides was developed at room temperature The catalytic method enabled easy access to various functionalized 2-aroylarom. carboxylic acid derivatives in good isolated yields. Based on our mechanistic studies, a Pd(II)/Pd(IV) catalytic cycle that involved aroyl radical intermediate was proposed for the reaction.

Palladium-Catalyzed Decarboxylative ortho-C(sp2)-H Aroylation of N-Sulfoximine Benzamides at Room Temperature. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

Synthesis of thiadiazine-1-oxide derivatives I [R1 = H, 4-Me, 3-OMe, etc.; R2 = i-Pr, 2-thienyl, Ph, etc.; R3 = 2-thienyl, Ph, 2-naphthyl, etc.] via Ir(III)-catalyzed C-H activation/cyclization of NH-sulfoximines with N-alkoxyamides as amidation reagents was developed. This one-pot cascade protocol tolerated diverse functional groups and readily constructed various heterocyclic frameworks in moderate to good yield.

Iridium(III)-Catalyzed C-H Amidation/Cyclization of NH-Sulfoximines with N-Alkoxyamides: Formation of Thiadiazine-1-Oxides. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

A novel strategy for the N-arylation of NH-sulfoximines has been developed by merging nickel catalysis and electrochem. (in an undivided cell), thereby providing a practical method for the construction of sulfoximine derivatives Paired electrolysis is employed in this protocol, so a sacrificial anode is not required. Owing to the mild reaction conditions, excellent functional group tolerance and yield are achieved. A preliminary mechanistic study indicates that the anodic oxidation of a NiII species is crucial to promote the reductive elimination of a C-N bond from the resulting NiIII species at room temperature

Nickel-Catalyzed N-Arylation of NH-Sulfoximines with Aryl Halides via Paired Electrolysis. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

(S-Methylsulfonimidoyl)benzene (BD302898) is a building block containing a sulfoximine group. Several CDK and ATR inhibitors have exemplified the utilization of the NH sulfoximine group as abioisostere for a sulfonamide group to overcome the main project hurdles of aqueous solubility, sulfonamide-mediated off-target activity and IP. Moreover, its NH group could be expediently further functionalized through Buchwald-Hartwig coupling reaction and multifarious nucleophilic reactions.. Recommended Products is: 83730-53-4 and 1621962-30-8.

A mild and facile Cp*Rh(III)-catalyzed C-H activation and intramol. cascade annulation protocol has been proposed for the furnishing of highly fused isochromeno-1,2-benzothiazines I (R1 = H, 2-Me, 2-F, 4-Br, 3-OMe, (CH2)4, etc.; R2 = Me, Et, Ph, Bn, etc.; R3 = H, 10-Me,10-OMe, 11-Cl, 11-F, etc.) scaffolds using S-phenylsulfoximides R4C6H4S(O)(=NH)(R2) and 4-diazoisochroman-3-imine II (R5 = H, 7-Me, 6-OMe, 7-OMe, 6-Cl, etc.) as substrates under room temperature This method features diverse substituents and functional groups tolerance and relatively mild reaction conditions with moderate to excellent yields. Addnl., retentive configuration of sulfoximides in the conversion has been verified.

Sulfoximines-assisted Rh(III)-catalyzed C-H activation and intramolecular annulation for the synthesis of fused isochromeno-1,2-benzothiazines scaffolds under room temperature. Recommended basis is Sulfoximine, Bioisosteric. Products is: https://www.ambeed.com/products/50578-18-2.html, 145026-07-9

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Tankam, Theeranon; Srisa, Jakkrit; Sukwattanasinitt, Mongkol; Wacharasindhu, Sumrit published the artcile< Microwave-Enhanced On-Water Amination of 2-Mercaptobenzoxazoles To Prepare 2-Aminobenzoxazoles>, Computed Properties of 13451-78-0, the main research area is microwave irradiation water amination mercaptobenzoxazole; aminobenzoxazole preparation green chem.

In this work, we developed a catalyst-free amination of 2-mercaptobenzoxazoles on water under microwave irradiation The product, 2-aminobenzoxazoles, was successfully produced via direct amination with various amines in moderate to high yields. The formal synthesis of Suvorexant, a medication for the treatment of insomnia, was accomplished using a developed amination process. The reaction was completed in an hour at 100-150° in a microwave reactor without the use of external catalyst or additive. Key benefits of this process include an on-water reaction, short reaction time, being scalable and catalyst-free, and use of 2-mercaptobenzoxazoles as an inexpensive starting material having low environmental impact in its preparation

Journal of Organic Chemistry published new progress about Amination. 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, Computed Properties of 13451-78-0.

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Wan, Jin-Lin; Huang, Jing-Mei published the artcile< Bromide-Catalyzed Electrochemical Csp3-H Oxidation of Acetonitrile: Stereoselective Synthesis of Heteroaryl Vinyl Sulfides>, Computed Properties of 13451-78-0, the main research area is heteroaryl vinyl sulfide preparation electrochem diastereoselective; acetonitrile heteroaryl thiol oxidative cross coupling reaction bromide catalyst.

An electrochem. oxidative C-H/S-H cross-coupling reaction between acetonitrile and heteroaryl thiols e.g., 1,3-benzoxazole-2-thiol has been developed. Me4NBr is employed as a redox catalyst to oxidize both the Csp3-H of acetonitrile and S-H of heteroaryl thiols. Heteroaryl vinyl sulfides e.g., I were afforded under metal-free and oxidant-free reaction conditions in good yields and stereoselectivities with excellent functional group tolerance. The synthetic applicability of the electrochem. method was further highlighted by its easy scalability.

Advanced Synthesis & Catalysis published new progress about Acetonitriles Role: RCT (Reactant), RACT (Reactant or Reagent). 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, Computed Properties of 13451-78-0.

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Liu, Xing; Liu, Min; Xu, Wan; Zeng, Meng-Tian; Zhu, Hui; Chang, Cai-Zhu; Dong, Zhi-Bing published the artcile< An environmentally benign and efficient synthesis of substituted benzothiazole-2-thiols, benzoxazole-2-thiols, and benzimidazoline-2-thiones in water>, Recommanded Product: 5-Fluorobenzo[d]oxazole-2-thiol, the main research area is benzothiazole thiol green preparation; aminothiol tetramethylthiuram disulfide cyclization; benzoxazole thiol green preparation; aminoalc tetramethylthiuram disulfide cyclization; benzimidazoline thione green preparation; diamine tetramethylthiuram disulfide cyclization.

An efficient and practical method for the one-step synthesis of benzothiazole-2-thiols I [R = H, 5-Cl; X = S], benzoxazole-2-thiols I [R = H, 5-Me, 5-Br, etc.; X = O] and benzimidazoline-2-thiones such as II by cyclization of 2-aminothiophenols, 2-aminophenols, and 1,2-phenylenediamines with tetramethylthiuram disulfide (TMTD) in water was described. This method was also used for the synthesis of 4,5-dihydro-thiazole-2-thiol, 4,5-dihydro-oxazole-2-thiol and 1,3-ethylenethiourea from their corresponding aliphatic amines and (TMTD). The features of this method included metal/ligand-free, excellent yield, short reaction time and broad substrate scope. The method provided a facile and convenient preparation of some potentially biol. active compounds

Green Chemistry published new progress about Amino alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, Recommanded Product: 5-Fluorobenzo[d]oxazole-2-thiol.

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Murray, Christopher W.; Berdini, Valerio; Buck, Ildiko M.; Carr, Maria E.; Cleasby, Anne; Coyle, Joseph E.; Curry, Jayne E.; Day, James E. H.; Day, Phillip J.; Hearn, Keisha; Iqbal, Aman; Lee, Lydia Y. W.; Martins, Vanessa; Mortenson, Paul N.; Munck, Joanne M.; Page, Lee W.; Patel, Sahil; Roomans, Susan; Smith, Kirsten; Tamanini, Emiliano; Saxty, Gordon published the artcile< Fragment-Based Discovery of Potent and Selective DDR1/2 Inhibitors>, Safety of 5-Fluorobenzo[d]oxazole-2-thiol, the main research area is DDR inhibitor antitumor oral; back to front kinase design; discoidin domain receptor; fragment-based drug design.

The DDR1 and DDR2 receptor tyrosine kinases are activated by extracellular collagen and have been implicated in a number of human diseases including cancer. We performed a fragment-based screen against DDR1 and identified fragments that bound either at the hinge or in the back pocket associated with the DFG-out conformation of the kinase. Modeling based on crystal structures of potent kinase inhibitors facilitated the “”back-to-front”” design of potent DDR1/2 inhibitors that incorporated one of the DFG-out fragments. Further optimization led to low nanomolar, orally bioavailable inhibitors that were selective for DDR1 and DDR2. The inhibitors were shown to potently inhibit DDR2 activity in cells but in contrast to unselective inhibitors such as dasatinib, they did not inhibit proliferation of mutant DDR2 lung SCC cell lines.

ACS Medicinal Chemistry Letters published new progress about Conformation. 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, Safety of 5-Fluorobenzo[d]oxazole-2-thiol.

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem

Wang, Guang-cheng; Wang, Jing; Li, Lu-yao; Chen, Shan; Peng, Ya-ping; Xie, Zhen-zhen; Chen, Ming; Deng, Bin; Li, Wen-biao published the artcile< Synthesis of N-aryl-2-aminobenzoxazoles from substituted benzoxazole-2-thiol and 2-chloro-N-arylacetamides in KOH-DMF system>, HPLC of Formula: 13451-78-0, the main research area is aminobenzoxazole aryl preparation; benzoxazole thiol arylacetamide chloro condensation.

A simple and novel method for the synthesis of N-aryl-2-aminobenzoxazoles I [R1 = H, 5-F, 6-Me, etc. ; R2 = 4-Cl, 2,4-di-Me, 4-OPh, etc.] from substituted benzoxazole-2-thiols II and 2-chloro-N-arylacetamides R2C6H4NHC(O)CH2Cl in KOH-DMF system has been developed. The present protocol provides an attractive approach to access various N-aryl-2-aminobenzoxazoles I in moderate to good yields without using transition metal catalyst under very mild reaction condition.

Heterocycles published new progress about Acetamides Role: RCT (Reactant), RACT (Reactant or Reagent). 13451-78-0 belongs to class benzoxazole, and the molecular formula is C7H4FNOS, HPLC of Formula: 13451-78-0.

Referemce:
Benzoxazole – Wikipedia,
Benzoxazole | C7H5NO – PubChem