100160-75-6

Upstream product

• 67-56-1 methanol 
• 2033-24-1 cycl-isopropylidene malonate 
• 5728-52-9 (4-biphenylyl)acetic acid 
• 31603-77-7 4-biphenylacetonitrile 
• 96-32-2 bromoacetic acid methyl ester 

Downstream Products

• 149709-62-6 α-ethyl (αR,γS)-γ-<(3-carboxy-1-oxopropyl)amino>-α-methyl<1,1'-biphenyl>-4-pentanoate 
• 752174-62-2 (2R,4S)-4-amino-5-biphenyl-4-yl-2-methylpentanoic acid ethyl ester 

Relevant academic research and scientific papers

SACUBITRIL INTERMEDIATE AND PREPARATION METHOD THEREOF

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.

Sacubitril intermediate and preparation method of sacubitril intermediate and sacubitril

The invention discloses a sacubitril intermediate and a preparation method of the sacubitril intermediate and sacubitril, and belongs to the technical field of organic synthesis of drugs. On one hand, the invention discloses a novel compound-sacubitril intermediate compound B and a preparation method thereof, and on the other hand, the invention discloses a novel preparation method of the sacubitril. The sacubitril intermediate and the preparation method of the sacubitril intermediate and the sacubitril have the following advantages that the synthesizing route is short, the product can be prepared only through four steps of chemical reactions, and the steps of existing patent routes all exceed nine steps; the dicarbonyl compound is prepared through Reformasky condensation supplied by the method, and the cost is low; a first chiral center is introduced by fully utilizing a chiral compound L-(S)-ethyl lactate which is low in cost and easy to obtain in the natural world, and the cost is low; a second chiral center is constructed through a biological enzyme catalysis technique, the optical selectivity reaches up to 99.9%, the quality is good, and the cost is low. By means of the technological means, the total yield of the prepared sacubitril is increased, and the quality of the sacubitril is improved.

ESTERS AND AMIDES AS PLA2 INHIBITORS

The present invention relates to a novel fatty acid derivative of formula (I), wherein R1 is acyl group; R2 is acyl(lower)alkyl; R3 is hydrogen, aryl(lower)alkyl, etc.; R4 is acyl(lower)alkyl; and X is —O—, —NH—