CAS: 486460-00-8; (R)-3-((Tert-Butoxycarbonyl)Amino)-4-(2,4,5-Trifluorophenyl)Butanoic Acid

上下游产品

CAS号936630-57-8 (R)-3-氨基-4-(2,4... | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号1048703-14-5 (R)-tert-butyl ... | CAS号881995-73-9 Benzenebutanoic... | CAS号881995-69-3 (R)-3-氨基-4-(2,4... | CAS号1152439-74-1 ethyl (R)-3-ter... | CAS号1204818-19-8 (R)-3-氨基-4-(2,4... | CAS号486460-32-6 西他列汀

Tert-Butyl N-[(2S)-1-(2,4,5-Trifluorophenyl)Pent-4-En-2-Yl]Carbamate置于potassium Permanganate体系中,用 丙酮 作为反应溶剂,化学反应 3.0H,以89%的收率获得产物boc-(R)-3-氨基-4-(2,4,5-三氟苯基)丁酸
参考文献:一种西他列汀中间体的制备方法
标题:一种西他列汀中间体的制备方法
摘要:本发明公开了一种西他列汀中间体的制备方法,属于药物合成领域,该制备方法的步骤为(1)开环反应:在四氢呋喃与甲基叔丁基醚的介质中,温度为零下20oc至零下50°C,以氯化亚铜为催化剂,2,4,5‑三氟溴苯与格式试剂rmgx,其中r为异丙基,X为卤素发生格林尼亚反应,反应生成的化合物再与如式3所示的化合物发生开环反应,得到如式4所示的化合物;(2)氧化反应:如式4所示的化合物与高锰酸钾在丙酮介质中发生氧化反应,用还原剂亚硫酸钠,亚硫酸氢钠淬灭,中和,甲基叔丁基醚萃取,得到西他列汀中间体.该方法成本低,收率高,工艺成熟,适合工业化生产.

专利信息

专利号:US-11965193-B2
优先权日:2017-07-11
标题:Use of stereoselective transaminase in asymmetric synthesis of chiral amine
发明人：CHENG ZHANBING; ZHANG TAO; TIAN ZHENHUA; DING SHAONAN
权利人:ABIOCHEM BIOTECHNOLOGY CO LTD
摘要:Use of a stereoselective transaminase in the asymmetric synthesis of a chiral amine. In particular, provided is use of a polypeptide in the production of a chiral amine or a downstream product using a chiral amine as a precursor. Further provided is a method for producing a chiral amine, comprising culturing a strain expressing the polypeptide so as to obtain a chiral amine. Further provided are novel prochiral compounds, a chiral amine production strain and a method for constructing the chiral amine production strain. The stereoselective transaminase has a broad substrate spectrum and thus has a broad application potential in the preparation of a chiral amine.

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-2009156465-A1
优先权日:2005-12-30
标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors
发明人：SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND
权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND
摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

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-8765668-B2
优先权日:2010-06-04
标 题 :Methods of synthesis of β-aminobutyryl substituted compounds
发明人：STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO
权利人:STERK DAMJAN; USTAR MATJAZ; ZLICAR MARKO; LEK PHARMACEUTICALS
摘要:The present invention relates to process to prepare β-aminobutyryl compounds having β-amino acid core structural moieties and optionally having γ-phenyl and/or heterocyclic structural moieties. Such compounds are useful as key structure framework of modern drug chemistry.

专利号:US-2009192326-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: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.