专利号:US-7977480-B2 优先权日:2007-12-10 标 题:Synthesis of paliperidone 发明人:BARTL JIRI; KRAJCOVIC JOZEF; BENOVSKY PETR 权利人:SYNTHON BV 摘要:A 9-hydroxy or 9-acyloxy group can be added to a pyridopyrimidinone ring structure by a process comprising acylating a compound of formula (5) under Vilsmeier-Haack or Friedel-Crafts conditions to form a compound (6); and transforming with a peroxo-compound to obtain the compound (1). n nR represents hydrogen or a C1-C20 acyl group. The process is useful in the synthesis of paliperidone and derivatives.
专利号:US-2008214809-A1 优先权日:2006-08-23 标 题 :Process for the synthesis of CMHTP and intermediates thereof 发明人:DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI; PILARSKY GIDEON 权利人:DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI; PILARSKY GIDEON 摘要:The present invention provides processes of preparing 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone, wherein the processes use 3-(2-chloroethyl)-2-methyl-9-benzyloxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMBP) and/or 3-(2-chloroethyl)-2-methyl-9-hydroxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) having phosphorus at least partially removed as the intermediate.
专利号:US-7820816-B2 优先权日:2006-08-23 标题:Process for the synthesis of CMHTP and intermediates thereof 发明人:DOLITZKY BEN-ZION; SHAPIRO EVGENY; INI SANTIAGO; SHMUELY YARON; LANCRY ELI 权利人:TEVA PHARMA 摘要:The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.
专利号:US-11667666-B2 优先权日:2020-01-20 标题 :Methods and compositions for treatment of cancer 发明人:SINGHAL ANUJ 权利人:CFD RES CORPORATION 摘要:In an aspect, the disclosure pertains to inhibitors of ANGPTL4; synthesis methods for making disclosed compounds; pharmaceutical compositions comprising disclosed compounds; methods of treating disorders of uncontrolled cellular proliferation, e.g., a cancer; and methods of treating a disease associated with an ANGPTL4 dysfunction using disclosed compounds and pharmaceutical compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:WO-2009074333-A1 优先权日:2007-12-10 标 题 :Synthesis of paliperidone
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合成参考文献
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