CAS: 767340-03-4; (2Z)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-Dihydro[1,2,4]Triazolo[4,3-A]Pyrazine-7(8H)-Yl]-1-(2,4,5-Trifluorophenyl)But-2-En-2-Amine

上下游产品

(2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氢-[1,2,4]三唑并[4,3-A]吡嗪-7-(8H)-基]-1-(2,4,5-三氟苯基)丁-2-酮 1-(3-(Trifluoromethyl)-5,6-Dihydro-[1,2,4]Triazolo[4,3-A]Pyrazin-7(8H)-yl)-4-(2,4,5-Trifluorophenyl)Butane-1,3-Dione 764667-65-4

3-三氟甲基-5,6,7,8-四氢-1,2,4-三唑并[4,3-A]吡嗪盐酸盐置于ammonium Acetate,氨体系中,用 甲醇,异丁酰胺,水 作为反应溶剂,化学反应 7.0H,反应生成 (2Z)-4-氧代-4-[3-(三氟甲基)-5,6-二氢-[1,2,4]三唑并[4,3-A]吡嗪-7(8H)-基]-1-(2,4,5-三氟苯基)丁-2-烯-2-胺
参考文献: Novel Crystalline Forms Of A Phosphoric Acid Salt Of A Dipeptidyl Peptidase-Iv Inhibitor[fr] Nouvelles Formes Cristallines D'Un Sel D'Acide Phosphorique D'Un Inhibiteur De Dipeptidyl Peptidase-Iv
标题: Novel Crystalline Forms Of A Phosphoric Acid Salt Of A Dipeptidyl Peptidase-Iv Inhibitor[fr] Nouvelles Formes Cristallines D'Un Sel D'Acide Phosphorique D'Un Inhibiteur De Dipeptidyl Peptidase-Iv

专利信息

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.

专利号:US-8476437-B2
优先权日:2008-08-27
标题:Process for preparation of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro [1,2,4]-triazolo[4,3-a]pyrazin-7(8H)-yl]-l-(2,4,5-trifluorophenyl)butan-2-amine and new impurities in preparation thereof
发明人：KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD
权利人:KOTHARI HIMANSHU MADHUSUDAN; DAVE MAYANK GHANSHYAMBHAI; PANDEY BIPIN; SHUKLA BHAVIN SHRIPRASAD; CADILA HEALTHCARE LTD
摘要:The present invention relates to synthesis of β-amino acid derivatives of formula (I) and its salts of formula (Ia) by a novel process. The process comprises the reduction of a protected or unprotected prochiral β-amino acrylic acid or derivative there of, by using borane containing reducing agents at atmospheric pressure. The resulting racemic β-amino compound is resolved to a pure stereoisomer of formula (I), specifically to (2R)-4-oxo-4-[3-Ctrifluoromethyl)-5,6-dihydrol[1,2,4]triazolo[4,3-alpyrazin-7(8H)-yl]-1-(2,4,4-trifluorophenyl)butan-2-amine. In an embodiment the invention disclosed polymorphic forms of formula (I), phosphate salt of formula (I) and also a Dibenzoyl-L-tartaric acid salt of formula (I).

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-7495123-B2
优先权日:2004-04-05
标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives
发明人：XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE
权利人:SOLVIAS AG; MERCK & CO INC
摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

专利号:US-11174266-B2
优先权日:2018-02-13
标 题 :Efficient process for the preparation of sitagliptin
发明人：SHI TERRY; LOU SAM; DE LUCCHI OTTORINO; PADOVAN PIERLUIGI
权利人: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.