20973-90-4Relevant academic research and scientific papers
Regioselective, Diastereoselective, and Enantioselective One-Pot Tandem Reaction Based on an in Situ Formed Reductant: Preparation of 2,3-Disubstituted 1,5-Benzodiazepine
Yang, Gao-Feng,Li, Guang-Xun,Huang, Jin,Fu, Ding-Qiang,Nie, Xiao-Kang,Cui, Xin,Zhao, Jin-Zhong,Tang, Zhuo
, p. 5110 - 5119 (2021/04/12)
The 1,5-benzodiazepines are important skeletons frequently contained in medicinal chemistry. Herein, we described an unexpected tandem cyclization/transfer hydrogenation reaction for obtaining chiral 2,3-disubstituted 1,5-benzodiazepines. The enolizable aryl aldehydes were chosen as substrates to react with symmetric and unsymmetric o-phenylenediamines. The unforeseen tandem reaction occurred among many possible latent side reactions under chiral phosphoric acid catalysis and affords the corresponding products in moderate yields and regioselectivities, good diastereoselectivities, and enantiomeric ratio (up to 99:1).
THERAPEUTIC COMPOUNDS
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Paragraph 0400; 0401, (2018/08/30)
The invention provides compounds of formula Ia′, Ib′, Ic′, and Id′: and pharmaceutically acceptable salts thereof, wherein the variables A, R6, R7, R8, R9, Rx, L, X, Y, and Z have the meaning as described herein. The compounds are useful for reducing endoplasmic reticulum stress and for producing analgesia in an animal.
Imidazolo-, oxazolo-, and thiazolopyrimidine modulators of TRPV1
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Page/Page column 18; 19, (2009/07/03)
Certain TRPV1-modulating imidazolo-, oxazolo-, and thiazolopyrimdine compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPV1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.
Nitrogen-heterocyclic compound and process for production thereof
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Page column 15, (2010/01/30)
A nitrogen-heterocyclic compound is provided which is represented by General Formula (1): where R1and R2are independently hydrogen, an alkyl group, an aryl group, or a heteroaryl group; R3is hydrogen or an aryl group; Rsu
Palladium/P(t-Bu)3-catalyzed synthesis of aryl t-butyl ethers and application to the first synthesis of 4-chlorobenzofuran
Watanabe, Makoto,Nishiyama, Masakazu,Koie, Yasuyuki
, p. 8837 - 8840 (2007/10/03)
Pd/P(t-Bu)3 catalyzed reaction of aryl halides with sodium t-butoxide effectively to give aryl t-butyl ethers. The high catalytic activity realized the formation of aryl t-butyl ethers from not only electron-deficient aryl halides but also electron-rich aryl halides. Moreover, the first synthesis of 4-chlorobenzofuran was attained utilizing the selective mono-t-butoxylation of aryl dihalide.
A facile approach to arylacetaldehydes via polymeric palladium catalyst
Zhuangyu,Yi,Honwen,Tsi-yu
, p. 539 - 542 (2007/10/02)
Several arylacetaldehydes 5 were synthesized in moderate yields via Heck reaction of acrylamide (1) with substituted iodobenzenes 2 in the presence of the polymeric catalyst (P)-phenyl-(1,10-phenanthroline)-palladium(0) [(P)-ph-phen·Pd(0)] followed by Hofmann reaction and subsequent hydrolysis.
