- Preparation method of neprilysin inhibitor intermediate
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The invention discloses a preparation method for an enkephalinase inhibitor intermediate. According to the preparation method, a target compound with a formula I as described in the specification is prepared by using a compound as shown in a formula IV which is described in the specification as an initial material through a reaction with few steps, wherein the compound with the formula I can be used for preparation of an enkephalinase inhibitor drug namely Sacubtril. In the formula I and the formula IV, R is selected from the group consisting of H, methyl, ethyl or other lower alkyl.
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Paragraph 0036-0037; 0039; 0041; 0043-0044; 0046; 0048
(2020/10/04)
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- Method for preparing sacubitril and intermediate thereof
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The invention provides a method for preparing sacubitril and an intermediate thereof and belongs to the field of medicine synthesis. The method comprises the following steps: by taking a compound I asa raw material, carrying out an asymmetric reduction reaction under the action of a chiral metallic catalyst so as to obtain an intermediate; finally carrying out a simple synthesis step, thereby obtaining a target product sacubitril. The method is short in synthesis route, easy to implement, high in reaction yield, good in diastereoselectivity, and capable of avoiding relatively tedious aftertreatment steps, and reducing the production cost of the sacubitril while the production efficiency of the sacubitril is improved.
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Paragraph 0080-0082
(2019/03/24)
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- SACUBITRIL INTERMEDIATE AND PREPARATION METHOD THEREOF
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The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril. The method disclosed herein has advantages of easily obtained raw materials, simple preparation process, low cost, environment friendly, and etc., which is very suitable for industrial production.
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- NEW PROCESS AND INTERMEDIATES
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The present invention relates to a new chemical synthesis, intermediates and catalysts useful for the preparation of the neprilysin (NEP) inhibitor sacubitril. It further relates to new intermediate compounds and their use for said new chemical synthesis route.
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- Sacubitril intermediate and preparation method thereof
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The invention relates to a sacubitril intermediate and a preparation method thereof, the sacubitril intermediate is a compound shown as formula (04), and the sacubitril intermediate is prepared by deprotection reaction of a compound shown as formula (03). Further, the invention also provides the preparation method of the compound shown as the formula (04) as the intermediate. The method has the advantages of easy availability of raw materials, simple process, economy and environmental protection, and the like, and is very suitable for industrial production.
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