专利号:US-6093825-A 优先权日:1998-05-27 标 题:Methods for preparation of 1,2-dihydroquinolines 发明人:BENDER REINHOLD H W; EDWARDS JAMES P; JONES TODD K 权利人:AMERICAN HOME PROD; LIGAND PHARM INC 摘要:Methods for conversion of anilines to 1,2-dihydroquinolines. 1,2-dihydroquinoliiies are generated from combining an aniline, a silylating agent, and further condensing with a ketone in the presence of a catalyst. In one aspect, the silylation of the aniline may be performed in a one-step synthesis by adding the silylating, agent to the same reaction vessel as the ketone, aniline, and catalyst. In a second aspect, the 1,2-dihydroquinoline is generated in a two-step synthesis where an N-silyl aniline is formed prior to the addition of the ketone and catalyst.
专利号:US-9217012-B2 优先权日:2009-04-08 标题 :Inhibitors of protein tyrosine phosphatases 发明人:ZHANG ZHONG-YIN; ZHANG SHENG 权利人:ZHANG ZHONG-YIN; ZHANG SHENG; UNIV INDIANA RES & TECH CORP 摘要:Disclosed herein are compounds that selectively inhibit members of the PTP family of enzymes. Synthesized compounds demonstrated selective inhibition of TC-PTP. Also provided are methods of using the compounds and formulations containing the compounds. Also described is a fluorescence-tagged combinatorial library synthesis and screening method. And methods of using these compounds to effect enzyme activity both in cells and in vitro as well as method of using these compounds to treat diseases in human and animals.
专利号:CN-103880740-B 优先权日:2014-04-14 标题 :Synthesis of 4-nitro-3-hydroxy-2-pyridinecarboxylic acid
专利号:CN-103880740-A 优先权日:2014-04-14 标 题:Synthesis of 4-nitro-3-hydroxy-2-pyridinecarboxylic acid
专利号:RU-2099341-C1 优先权日:1989-09-13 标题:Tetrahydroimidazo-[1,4]-benzodiazepines or their pharmaceutically acceptable salts or stereoisomers, a method of their synthesis, intermediate compounds for their synthesis and antiviral composition
专利号:US-9695191-B2 优先权日:2009-08-05 标题 :Conformationally constrained, fully synthetic macrocyclic compounds 发明人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN 权利人:OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; LACH FRANCK; LUTHER ANATOL; MARX KARSTEN; MÖHLE KERSTIN; POLYPHOR AG 摘要:Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT 2B (5-HT 2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.
[参考文献]: Esther C Y Woon, Et Al. One-Pot Tandem Hurtley-Retro-Claisen-Cyclisation Reactions In The Synthesis Of 3-Substituted Analogues Of 5-Aminoisoquinolin-1-One (5-Aiq), A Water-Soluble Inhibitor Of Parps. Bioorg Med Chem. 2013 Sep 1;21(17):5218-27.
合成参考文献
摘要:Prager, R. H.; Williams, C. M., Science of Synthesis, (2005) 15, 1040.