CAS: 1029877-94-8; (R)-2-((6-(3-Aminopiperidin-1-yl)-3-Methyl-2,4-Dioxo-3,4-Dihydropyrimidin-1(2H)-yl)Methyl)-4-Fluorobenzonitrile Succinate

烟酰胺置于吡啶,Palladium On Carbon Type-K,氢气,Ru-(Cf3Co2)2{(S)-Phanephos},Potassium Carbonate,[双(三氟乙酰氧基)碘]苯,Potassium Bromide体系中,用 四氢呋喃,甲醇,乙醇,水,异丙醇 用作溶剂,20.0~65.0 °C,1.0 Mpa 条件下,反应 63.0H,反应生成曲格列汀琥珀酸盐
参考文献:阿格列汀的不对称合成工艺的开发和放大
标题:阿格列汀的不对称合成工艺的开发和放大
摘要:阿格列汀(1)苯甲酸酯是一种有效的,高度选择性的丝氨酸蛋白酶二肽基肽酶iv抑制剂,已获美国fda批准用于治疗2型糖尿病.在此,我们报告了一种更具成本效益的方法,其中包括钌催化的不对称氢化反应,然后进行2-(((6-氯-3-甲基-2,4-二氧代-3,4-二氢嘧啶-1(2 H)-基)甲基)苄腈(10)在后期引入手性氨基部分.在温和且特殊的条件下,使用廉价且容易获得的烟酰胺(6)制备手性氨基哌啶核和碘代苯二乙酸盐(pida),使我们可以使用1 具有极佳的总产量和可与原始工艺生产的产品相媲美的质量.
Doi:10.1021/acs.Oprd.0C00544

专利信息

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-2018370905-A1
优先权日:2013-04-05
标题:Compounds Useful for the Treatment of Metabolic Disorders and Synthesis of the Same

专利号:US-2016046560-A1
优先权日:2013-04-05
标题 :Compounds useful for the treatment of metabolic disorders and synthesis of the same

专利号:CN-107445887-A
优先权日:2017-08-28
标 题:Application of the asymmetric hydrogenation in the synthesis of bent Ge Lieting intermediates

专利号:CN-119614531-A
优先权日:2024-12-09
标 题:Application of an R-aminotransferase and its mutants in asymmetric synthesis of chiral amine compounds

专利号:CN-119614650-A
优先权日:2024-12-09
标 题:R-aminotransferase and its application in asymmetric synthesis of chiral N-heterocyclic amines