CAS: 881995-69-3; Benzenebutanoic Acid, β-Amino-2,4,5-Trifluoro-, Methyl Ester, (βr)

上下游产品

CAS号486460-00-8 (3R)-N-叔丁氧羰基-3-... | CAS号486460-32-6 西他列汀

Boc-(R)-3-氨基-4-(2,4,5-三氟苯基)丁酸置于盐酸,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 二氯甲烷,水 作为反应溶剂,化学反应生成 西他列汀-Int A8
参考文献:西他列汀游离碱及西他列汀磷酸盐一水合物的合成方法
标题:西他列汀游离碱及西他列汀磷酸盐一水合物的合成方法
摘要:本发明涉及一种西他列汀游离碱及西他列汀磷酸盐一水合物的合成方法,本发明通过除去干燥的hobt或改为hobt水合物,在工艺中除去溶剂dmf以及在生产过程中使用易于回收的简单溶剂,降低了生产成本,提高了反应安全性;本发明从式2化合物到式6化合物的原位法工艺可以提高产量并减少操作步骤,用用其他溶剂代替甲醇或异丙醇ipa,从而避免了产生式7,式8和式9所示的杂质,从而大大提高了产物纯度及收率,西格列汀游离碱的HPLC纯度在99%以上.

专利信息

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: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:WO-2013114173-A1
优先权日:2012-01-30
标题:A novel process for the preparation of sitagliptin
发明人：MALLELA SAMBHU PRASAD SARMA; HAVALE SHRIKANT HANUMANTAPPA; BODDEPALLI NAGABHUSHANA RAO; GUNJI NAGARJUNA; MOKKAPATI BHAVANI SANKAR
权利人:SMILAX LAB LTD; MALLELA SAMBHU PRASAD SARMA; HAVALE SHRIKANT HANUMANTAPPA; BODDEPALLI NAGABHUSHANA RAO; GUNJI NAGARJUNA; MOKKAPATI BHAVANI SANKAR
摘要:The present invention is directed to a process for the preparation of enantiomerically enriched β-amino acid derivatives which are important chiral building blocks and intermediates in pharmaceuticals. More specifically, the invention pertains to a novel process for practically convenient and economically producing enantiomerically enriched β-amino acid derivatives which are useful for the synthesis of amide inhibitors of dipeptidyl peptidase IV like Sitagliptin, which have been used to treat type 2 diabetes.

专利号:WO-2023012819-A1
优先权日:2021-07-31
标 题 :Recombinant transaminase polypeptides
发明人：VENKATESAN SURYANARAYANAN; SINGH ANKITA; PANDE KAJAL; PRAHLAD DWARAKANATH; KULKARNI NAVEEN; SOKKAR PANDIAN; ASHOKAN ANISHA; SRINIVASAN MUDAMBI ROHIT
权利人:QUANTUMZYME LLP
摘要:The present invention provides recombinant transaminase polypeptides, fusion protein comprising the same and process of designing the same. Further, the present invention provides a process of preparing chiral amines catalyzed by the recombinant transaminase polypeptides. Also, the present invention provides uses of the recombinant transaminase polypeptides. The recombinant transaminases of the invention lead to reduced cost of synthesis of enantiopure chiral amines along with high yield and purity.

专利号:US-8524936-B2
优先权日:2011-05-18
标 题:Manufacturing process for sitagliptin from L-aspartic acid
发明人：SOUKUP MILAN
权利人:SOUKUP MILAN
摘要:The present invention relates to a novel manufacturing process of pharmaceutically active compound of formula I used as oral anti-diabetic drug. Starting from L-aspartic acid derivate of formula IV the invention describes preparation of the chiral (R)-β-amino acid of formula II known as a precursor in the synthesis of Sitagliptin (formula I).

专利号:CN-104805069-A
优先权日:2015-02-06
标 题:A kind of immobilized transaminase and its application in the synthesis of sitagliptin intermediate