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一种工艺、化合物的技术，应用在新工艺领域，能够解决不对称配体昂贵、总体反应成本影响、非立体选择性和立体选择性氢化反应经济角度不利等问题，达到反应步骤数量少、低成本的效果

Active Publication Date: 2015-11-04
SUZHOU NOVARTIS PHARMA TECHONOLOGY CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, commonly used asymmetric ligands are usually only available through complex synthetic routes and / or are very expensive, thus contributing significantly to the overall reaction cost
Therefore, large-scale non-stereoselective and stereoselective hydrogenation reactions are economically unfavorable

Method used

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Examples

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Embodiment 1

[0344] The following examples describe the synthesis of compounds under the general formula (3) category according to the following general reactions

[0345]

[0346] where X is halogen, preferably chlorine, or -O-R5, where R5 is C 1 -C 6 - alkyl, preferably tert-butyl; and wherein the compound of formula (4) is reacted with a biphenyl compound, preferably an activated biphenyl compound.

Embodiment 1A

[0347] Example 1A: (S)-1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-ol

[0348]

Embodiment 1A-1

[0349] Example 1A-1: (S)-1-([1,1'-biphenyl]-4-yl)-3-chloropropan-2-ol (laboratory scale)

[0350] Add 88g THF containing 4.94 magnesium powder to the 500ml four-necked bottle, and stir. In parallel, a solution of 46.6 g of 4-bromophenol in 88 g of THF was prepared. reaction system under vacuum and N 2 Heat to 35-45°C under air. A THF solution of a small amount of iodine and 25 ml of 4-bromophenol was added to the magnesium / THF mixture with stirring. Then, the remaining 4-bromophenol in THF was added at 35-45°C while maintaining the temperature. After the mixture was cooled, 3.81 g of cuprous iodide was added and the mixture was further cooled. Subsequently, a THF solution containing 22.2 g of (S)-epichlorohydrin in 30 g of THF was added at -15 to -20°C while maintaining the temperature. The mixture was then poured into 120.4 g of 4M hydrochloric acid and stirred. The mixture was then placed upright to separate the phases. The organic phase was collected and the aqueous ...

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Abstract

The invention relates to a new enantioselective process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a γ-amino-δ-biphenyl-α-methylalkanoic acid, or acid ester, backbone.

Description

Background technique [0001] The present invention relates to a new process for the generation of useful intermediates for the production of NEP inhibitors or prodrugs thereof, especially NEPs containing a gamma-amino-delta-biphenyl-alpha-methylalkanoic acid or ester backbone Inhibitors. [0002] Endogenous atrial natriuretic peptide (ANP), also known as atrial natriuretic factor (ANF), has diuretic, natriuretic, and vasodilatory functions in mammals. Native ANF peptides are metabolically inactivated, in particular by degrading enzymes that are recognized to correspond to neutral endopeptidases (NEP, EC 3.4.24.11), also causing metabolic inactivation of eg enkephalins. [0003] Biaryl-substituted phosphonic acid derivatives are known to be used as neutral endopeptidase (NEP) inhibitors, such as inhibitors of ANF-degrading enzymes in mammals, to prolong and potentiate by inhibiting the degradation of ANF to less active metabolites Diuretic, natriuretic and vasodilatory propert...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C215/20C07C213/00
CPCC07C269/04C07B2200/07C07C29/36C07C41/30C07C213/00C07C213/02C07C269/06C07C215/28C07C271/16C07C271/22C07C33/46C07C43/1782
Inventor 朱国良叶文发郑辉钱灵峰位军辉杨立军李运广罗力军
Owner SUZHOU NOVARTIS PHARMA TECHONOLOGY CO LTD
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