CAS: 486460-23-5; (R)-Tert-Butyl (4-Oxo-4-(3-(Trifluoromethyl)-5,6-Dihydro-[1,2,4]Triazolo[4,3-A]Pyrazin-7(8H)-yl)-1-(2,4,5-Trifluorophenyl)Butan-2-yl)Carbamate

上下游产品

3-trifluoromethyl-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine (3R)-3-[(1,1-dimethylethoxycarbonyl)amino]-4-(2,4,5-trifluorophenyl)butanoic acid tert-butyl dicarbonatedi-tert-butyl dicarbonate 2,4,5-trifluorobenzyl bromidesitagliptin phosphate (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine phosphate (R)-3-amino-4-(2,4,5-trifluorophenyl)butyric acid methyl ester (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine hydr°Chloride

📜Boc-L-蛋氨酸置于甲醇,Sodium Hypochlorite,Sodium Tetrahydroborate,正丁基锂,2,2,6,6-四甲基哌啶氧化物,碘,异丙基溴化镁,碳酸氢钠,1-羟基苯并三唑,盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺,三乙胺,Sodium Bromide,碘甲烷体系中,用 四氢呋喃,甲醇,二氯甲烷,水,乙腈 作为反应溶剂,化学反应 33.33H,反应生成 N-叔丁氧羰基-西他列汀
参考文献:Intermediates Of Sitagliptin And Preparation Process Thereof
标题:Intermediates Of Sitagliptin And Preparation Process Thereof
摘要:揭示了西他列汀的中间体,其制备过程以及利用这些中间体合成西他列汀的方法.西他列汀是通过使用手性氨基化合物作为原料合成的,无需通过手性不对称催化氢化建立手性中心,并且避免了高压氢化反应.

专利信息

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-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-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.

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:JP-6199556-B2
优先权日:2009-05-11
标题:Synthesis of sitagliptin

专利号:JP-2016029051-A
优先权日:2009-05-11
标题 :Synthesis of sitagliptin