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-8940749-B2 优先权日:2011-05-31 标题:Preparation of 3-[2-[4-((6-fluoro-1, 2-benzisoxazol-3-yl)-l-piperidinyl)-6, 7, 8, 9-tetrahydor-9-hydroxy-2-methyl-4H-pyrido[ 1, 2-A]-pyrimidin-4-one(paliperidone) and paliperidone palmitate 发明人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY 权利人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; NEELA PRAVEEN KUMAR; BATTHINI GURUSWAMY; VENKATA NARASIMHARAO TELAGAREDDY; RAVANABABU KOSIREDDY; SUDHEER KALLEPALLY 摘要:An improved process for the synthesis of 3-[2-[4-((6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one (Paliperidone) and Paliperidone Palmitate through a novel intermediate (2-Chloroethyl)-6,7,8,9-tetrahydro-2-methyl-9-hydroxy-4H-pyrido [1,2-a]pyrimidine-4-one Palmitate ester.
专利号:US-5001136-A 优先权日:1990-06-07 标 题 :Leukotriene-synthesis-inhibiting 2-substitutedmethylamino-5-(hydroxy or alkoxy)pyridines 发明人:WALKER FREDERICK J 权利人:PFIZER 摘要:2-substitutedmethylamino-amino 5-(hydroxy or alkoxy) pyridines and derivatives thereof are disclosed. The compounds are inhibitors of leukotriene synthesis and are therefore useful for the treatment of pulmonary, inflammatory, dermatological, allergic and cardiovascular diseases.
专利号:US-2006004188-A1 优先权日:2000-09-29 标 题:Intermediates and the synthesis of modified carbocyanine dyes and their conjugates
专利号:US-8653223-B2 优先权日:2008-04-16 标题:Transketalized compositions, synthesis, and applications 发明人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG 权利人:SELIFONOV SERGEY; GOETZ ADAM EDWARD; JING FENG; SEGETIS INC 摘要:Ketal compounds of the structure I n nand a method of preparation of the compound from polyols and oxocarboxylates, as well as uses thereof.