CAS: 74844-91-0; 1-(Tert-Butyl) 2-Methyl (2S,4R)-4-Hydroxypyrrolidine-1,2-Dicarboxylate

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CAS号24424-99-5 二碳酸二叔丁酯 | CAS号40216-83-9 L-羟脯氨酸甲酯盐酸盐 | CAS号13726-69-7 B°C-L-羟脯氨酸 | CAS号74-88-4 碘甲烷 | CAS号1499-56-5 (2S,4R)-4-羟基吡咯烷... | CAS号18107-18-1 (三甲硅烷)重氮甲烷 | CAS号186581-53-3 重氮甲烷 | CAS号1070-19-5 Carbonazidic ac... | CAS号51-35-4 L-羟脯氨酸 | CAS号336818-78-1 (2S,4R)-N-叔丁氧羰基... | CAS号487048-28-2 顺式-N-b°C-4-氰基-l... | CAS号317357-42-9 (2S,4s)-1-(叔丁氧基... | CAS号51-35-4 L-羟脯氨酸 | CAS号426844-76-0 (2S,4S)-1-B°C-2... | CAS号215918-21-1 (2S)-4,4-二氟-2-(... | CAS号191280-88-3 1-N-B°C-(2S,4S)... | CAS号487-79-6 海藻酸(mM/ml) | CAS号88043-21-4 N-B°C-反式-4-对甲苯磺... | CAS号83623-93-2 顺式-1-N-B°C-4-甲氧...

L-羟基脯氨酸置于氯化亚砜,三乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 28.5H,反应生成 N-Boc-反式-4-羟基-L-脯氨酸甲酯
参考文献:公斤级顺式-Lc15-0133酒石酸盐(一种有效的二肽基肽酶iv抑制剂)的合成
标题:公斤级顺式-Lc15-0133酒石酸盐(一种有效的二肽基肽酶iv抑制剂)的合成
摘要:(4S)-N-Boc-4-氟-1-脯氨酸甲酯(4)由以下反应顺序制备:反式-4-羟基-1-脯氨酸的酯化(2),Boc保护和氟化通过dast.的反应4与锂化二唑提供恶二唑基酮7.boc基团7脱保护,然后与溴乙酰溴偶联,得到溴化物9.9与过量的恶唑烷16的偶联反应提供了偶联产物17.出乎意料的是,17完全差向异构化为几乎1:1种混合物的顺式-和反式-17在这个阶段.所述的脱保护后n,O的-亚甲基缩醛基17使用氯化铵水溶液,结晶诱导动态分辨率(cidr)的顺式-和反式lc15-0133(的-混合物1中的酒石酸盐的形成过程中)提供顺式-Lc15-0133(1A)酒石酸盐,产率为83%(de> 98%).
DOI:10.1021/op800076R

专利信息

专利号:WO-2009152051-A1
优先权日:2008-06-12
标题:Synthesis of a macrocyclic hcv protease inhibitor
发明人：WANG PENG
权利人:PHENOMIX CORP; WANG PENG
摘要:The present invention provides a method of synthesis of a macrocyclic compound known as a potent inhibitor of a protease produced by the hepatitis C virus (HCV). Inhibition of the viral protease blocks assembly of mature viral particles in an infected mammalian host. The method of synthesis involves a ring-closing metathesis step using a ruthenium catalyst. Hydrogenation and boronate deprotection provide the HCV protease-inhibitory product.

专利号:US-2012095211-A1
优先权日:2010-09-22
标 题 :Substituted proline inhibitors of hepatitis c virus replication
发明人：BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D
权利人:BUCKMAN BRAD; NICHOLAS JOHN B; SEREBRYANY VLADIMIR; SEIWERT SCOTT D; INTERMUNE INC
摘要:The embodiments provide compounds of the general Formulae I, Ia, II, IIa, III, IIIa, IIIb, IV, IVa, IVb, V, Va, Vb, VI, VIa, VIb, and VIc, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition. The embodiments also provide methods for the synthesis of subject compounds and intermediates in the synthetic methods.

专利号:WO-2006100479-A1
优先权日:2005-03-22
标题:Methods for the synthesis of heteroaromatic compounds
发明人：KNIGHT DAVID W
权利人:UNIV CARDIFF; KNIGHT DAVID W
摘要:Methods of making heteroaromatic compounds comprising a 5- membered ring, and dihydro forms thereof, by a metal catalysed 5-endo-cyclisation of alkynes (acetylenes) are disclosed. The methods involve the use of a catalyst comprising a silver salt, more preferably a silver (I) salt, which is employed as a heterogeneous catalyst for the cyclisation reaction. The methods can produce different types of heteroaromatic compounds and are capable of producing highly substituted products, i.e. products in which the 5-membered ring is disubstituted, trisubstituted or, with further simple reactions, tetrasubstituted. The methods described herein generally the advantages that they use conditions and reagents that are benign, cheap and flexible and amenable to scale up, and in which the only by-product is water.

专利号:US-9175026-B2
优先权日:2011-03-23
标题:Synthesis of thioether containing trialkoxysilanes
发明人：GARRELL ROBIN L; TUCKER-SCHWARTZ ALEXANDER K
权利人:GARRELL ROBIN L; TUCKER-SCHWARTZ ALEXANDER K; UNIV CALIFORNIA
摘要:The invention relates to a radical-initiated thiol-ene or thiol-yne “clickâ€? reaction that provides a simple and efficient route to diverse trialkoxysilanes. Trialkoxysilanes made in this way are obtained in quantitative to near-quantitative yields with high purity without any or minimal purification. A wide range of functional groups is tolerated in this approach, and even complex alkenes click with the silane precursors. The modular nature of these radical-based thiol-ene or thiol-yne “clickâ€? reactions allows a wide variety of pendant groups to be coupled to silane compounds that can then be coupled to a wide variety surfaces in order to modify their material properties. Consequently, such radical initiated thiol-ene and thiol-yne reactions provide facile and efficient methods for preparing an enormous number of surface-active functional trialkoxysilanes.

专利号:US-9549921-B2
优先权日:2013-06-24
标 题:Heterocyclic compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

专利号:WO-2015173779-A1
优先权日:2014-05-16
标题:Process for the preparation of teneligliptin and its novel intermediates
发明人：DUBEY SUSHIL KUMAR; KUMAR NEERAJ; NARWAL SURESH; DUBEY SHAILENDRA KUMAR; KUMAR PRAMOD
权利人:MICRO LABS LTD
摘要:The present invention relates to a novel process for the preparation of Teneligliptin or its pharmaceutically acceptable salts and its hydrates thereof. The invention also relates to novel intermediates used in the synthesis of Teneligliptin and their preparation.