CAS: 157911-56-3; 1-(Bromomethyl)-2,4,5-Trifluorobenzene

相似化合物

1765-40-8 157911-55-2 151412-02-1

上下游产品

CAS号486460-09-7 B°C-D-2,4,5-三氟苯丙氨酸 | CAS号486460-00-8 (3R)-N-叔丁氧羰基-3-... | CAS号486460-08-6 (R)-N-叔丁氧羰基-2,4... | CAS号486460-32-6 西他列汀

2,4,5-三氟苯甲醇置于三溴化磷体系中,化学反应 4.0H,反应生成2,4,5-三氟苄基溴
参考文献:抗糖尿病西他列汀关键前体d-(2,4,5-三氟苯基)丙氨酸的生物催化逆合成方法
标题:抗糖尿病西他列汀关键前体d-(2,4,5-三氟苯基)丙氨酸的生物催化逆合成方法
摘要:在目标分子的逆合成分析中整合生物催化步骤具有多种优势,例如减少了过程的环境足迹,更温和,更安全的反应条件的可行性以及转化率的可及性,这些都是传统化学合成所面临的挑战.在此,描述了用于合成氟化d的六种化学酶促途径.-苯丙氨酸衍生物,重磅炸弹抗糖尿病药物西他列汀的前体.所有途径均从相同的醛前体开始,并且涉及至少一个生物催化步骤,包括还原胺化,转氨作用,脱氨,加氢胺化和烯烃还原.从醛中以2-5步获得目标分子,Ee高达99%以上,分离产率为36-62%.此外,作为一种途径的一部分,报道了肉桂酸衍生物完全生物催化转化为相应的d-苯丙氨酸(正式的d-选择性加氢胺化)的第一个例子.
Doi:10.1039/c9Gc01902B

专利信息

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:EP-2397141-A1
优先权日:2010-06-16
标 题:Process for the synthesis of beta-amino acids and derivatives thereof
权利人:LEK PHARMACEUTICALS
摘要:The present invention relates to a process for the preparation of β-amino acids and derivatives thereof, which is especially suited for gliptins and particularly sitagliptin. A key step makes use of suitably derivatized epoxides or aziridines, which owing to a chirality provides a source of chirality for intermediates which are suitable for building up β-amino acids and similar compounds, in particular in the construction of the sitagliptin molecule.

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:US-8471057-B2
优先权日:2009-09-27
标 题:Sitagliptin intermediates, preparation methods and uses thereof
发明人：ZHU GUOLIANG; ZHANG JIAN; YANG LIJUN; YAO QINGDAN; YING JIE
权利人:ZHU GUOLIANG; ZHANG JIAN; YANG LIJUN; YAO QINGDAN; YING JIE; ZHEJIANG JIUZHOU PHARM CO LTD
摘要:The present invention relates to Sitagliptin intermediate and preparation method and use thereof. The method comprises reacting compound of formula (II) and trifluorobromobenzene with a Grignard reagent by a Grignard reaction to obtain a compound of formula (I). Compound of formula (I) is a new intermediate compound for the synthesis of Sitagliptin. Compound of formula (I) can be easily used for preparing another important intermediate compound of formula (V) for the synthesis of Sitagliptin. The structures of the compounds mentioned above are as the following:

专利号:CN-115260166-A
优先权日:2022-07-13
标题 :A new chemical method for the efficient synthesis of S-217622

专利号:CN-115260166-B
优先权日:2022-07-13
标题 :A chemical method for the efficient synthesis of S-217622