专利号:WO-2023021529-A1 优先权日:2021-08-17 标题:Improved enzymatic synthesis of sitagliptin or its salts thereof 发明人:DATLA ANUPAMA; NAGRE PRASHANT; TAMORE JAGDISH; WADHAVANE SACHIN; MURALIDHARAN KRISHNA; TRIVIKRAM SREENATH 权利人:FERMENTA BIOTECH LTD 摘要:The present invention discloses an improved enzymatic synthesis of Sitalgiptin or its pharmaceutically acceptable salts in good yield and purity. The present invention provides novel intermediate (R)- 3-Acetamido-4-(2,4,5-Trifluorophenyl) butanoic acid (5).
专利号:WO-2024137329-A1 优先权日:2022-12-20 标 题:Methods for the synthesis of complement factor d inhibitors and intermediates thereof 发明人:HASHIMOTO AKIHIRO; TIPPARAJU SURESH KUMAR 权利人:ALEXION PHARMA INC 摘要:The present disclosure provides methods for the synthesis of complement factor D inhibitors and intermediates thereof.
专利号:US-8846916-B2 优先权日:2009-05-11 标题:Sitagliptin synthesis 发明人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH 权利人:GORE VINAYAK GOVIND; GADAKAR MAHESHKUMAR; BHOSLE PRIYANKA; SHINDE SURESH; GENERICS UK LTD 摘要:The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid.
专利号:US-10913747-B2 优先权日:2017-07-04 标题 :Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid 发明人:DE LUCCHI OTTORINO; PADOVAN PIERLUIGI; BRASOLA ELENA 权利人:FIS FABBRICA ITALIANA SINTETICI SPA; F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
专利号:WO-2009064476-A1 优先权日:2007-11-13 标 题 :Preparation of sitagliptin intermediate 发明人:PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 权利人:TEVA PHARMA; TEVA PHARMA; PERLMAN NURIT; ETINGER MARINA; NIDDAM-HILDESHEIM VALERIE; ABRAMOV MILI 摘要:Intermediate compounds in the synthesis of Sitagliptin, 3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and amino protected-3-amino-4-(2,4,5- trifluorophenyl)but-2-enoic acid alkyl ester, and the stereoselective reduction of these compound to give Synthon I, or the amino-protected Synthon I, are provided.
专利号:US-7468459-B2 优先权日:2003-03-19 标题:Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation 发明人:XIAO YI; ARMSTRONG III JOSEPH D; KRSKA SHANE W; NJOLITO EUGENIA; RIVERA NELO R; SUN YONGKUI; ROSNER THORSTEN 权利人:MERCK & CO INC 摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.
参考标题:Design And Synthesis Of Poly(Adp-Ribose) Polymerase Inhibitors: Impact Of Adenosine Pocket-Binding Motif Appendage To The 3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide On Potency And Selectivity 作者:Uday Kiran Velagapudi,Marie-France Langelier,Cristina Delgado-Martin,Morgan E. Diolaiti,Sietske Bakker,Alan Ashworth,Bhargav A. Patel,Xuwei Shao,John M. Pascal,Tanaji T. Talele |发布日期:2019.6.13 摘要:Poly(Adenosine 5'-Diphosphate-Ribose) Polymerase (Parp) Inhibitors Are A Class Of Anticancer Drugs That Block The Catalytic Activity Of Parp Proteins. Optimization Of Our Lead Compound 1 (( Z)-2-Benzylidene-3-Oxo-2,3-Dihydrobenzofuran-7-Carboxamide; Parp-1 Ic50 = 434 Nm) Led To A Tetrazolyl Analogue (51, Ic50 = 35 Nm) With Improved Inhibition. Isosteric Replacement Of The Tetrazole Ring With A Carboxyl