[EN] 3, 4 - SUBSTITUTED PIPERIDINE DERIVATIVES AS RENIN INHIBITORS<br/>[FR] DÉRIVÉS DE PIPÉRIDINE 3,4-SUBSTITUÉE CONVENANT COMME INHIBITEURS DE LA RÉNINE
申请人:MERCK FROSST CANADA LTD
公开号:WO2009140769A1
公开(公告)日:2009-11-26
The present invention relates to 3,4-substituted piperidinyl - based renin inhibitor compounds bearing at 4-position lsoqumolone and having the Formula (I) : The invention further relates to pharmaceutical compositions containing said compounds, as well as their use in treating cardiovascular events and renal insufficiency.
PROCESSES FOR PREPARING 4-METHYL-5-NONANONE AND 4-METHYL-5-NONANOL
申请人:Shin-Etsu Chemical Co., Ltd.
公开号:US20200199053A1
公开(公告)日:2020-06-25
The present invention provides a process for preparing 4-methyl-5-nonanone of the following formula (3), the process comprising at least a step of subjecting pentanoic anhydride of the following formula (1) and a 2-pentyl nucleophilic reagent of the following general formula (2), in which M represents Li, MgZ
1
, or ZnZ
1
, wherein Z
1
represents a halogen atom or a 2-pentyl group, to a nucleophilic substitution reaction to produce 4-methyl-5-nonanone (3), as well as a process for preparing 4-methyl-5-nonanol of the following formula (7), the process comprising at least steps of preparing 4-methyl-5-nonanone and subjecting the obtained 4-methyl-5-nonanone and a reducing agent to a reduction reaction to produce 4-methyl-5-nonanol (7).
Iterative Deoxypropionate Synthesis Based on a Copper-Mediated Directed Allylic Substitution: Formal Total Synthesis of Borrelidin (C3–C11 Fragment)
作者:Christian Herber、Bernhard Breit
DOI:10.1002/chem.200600343
日期:2006.8.25
alkylation strategies such as enolate reactivity as well as costs and problems associated with the chiral auxiliary. Practicability of this new method is demonstrated through application in natural product syntheses. Thus, an efficient synthesis of the northern part of the angiogenesis inhibitor borrelidin (28), the deoxypropionate building block 27, could be devised, representing a formal total synthesis
Phosphonium Salt-Promoted C2–H Functionalization of Heterocyclic <i>N</i>-Oxides
作者:Qian Ma、Yuze Shi、Dong Wang
DOI:10.1021/acs.orglett.3c03742
日期:2023.12.29
We report the development of a phosphonium salt as a remarkable activating agent that enables the direct conversion of C2–H bonds of a variety of heterocyclicN-oxides into C2–N, C2–O, or C2–S bonds with high efficiency. The phosphonium salt was prepared on a >150 g scale in a single step and is tolerant of multiple functionalities.
我们报告了鏻盐作为一种卓越的活化剂的发展,它能够将各种杂环N-氧化物的C2-H键直接高效地转化为C2-N、C2-O或C2-S键。鏻盐一步制备 >150 g 规模,并且具有多种功能。
Processes for preparing 4-methyl-5-nonanone and 4-methyl-5-nonanol
申请人:Shin-Etsu Chemical Co., Ltd.
公开号:US10882806B2
公开(公告)日:2021-01-05
The present invention provides a process for preparing 4-methyl-5-nonanone of the following formula (3), the process comprising at least a step of subjecting pentanoic anhydride of the following formula (1) and a 2-pentyl nucleophilic reagent of the following general formula (2), in which M represents Li, MgZ1, or ZnZ1, wherein Z1 represents a halogen atom or a 2-pentyl group, to a nucleophilic substitution reaction to produce 4-methyl-5-nonanone (3), as well as a process for preparing 4-methyl-5-nonanol of the following formula (7), the process comprising at least steps of preparing 4-methyl-5-nonanone and subjecting the obtained 4-methyl-5-nonanone and a reducing agent to a reduction reaction to produce 4-methyl-5-nonanol (7).