Preparation of (2R,3S)-3-benzamido-2-hydroxy-3-phenylpropionic acid methyl ester_Kain Industrial Additives
Background and overview[1] (2R,3S)-3-Benzoylamino-2-hydroxy-3-phenylpropionic acid methyl ester can be passed through 3-hydroxy-4-phenylazetidin-2-one (HPA) It is prepared in two steps and can be used to prepare paclitaxel. Paclitaxel is a mitotic inhibitor or spindle poison and is a new type of anti-microtubule drug. Preparation[1] Step a, preparation of 3-phenylisoserine methyl ester hydrochloride Dissolve 50g of 3-hydroxy-4-phenylazetidin-2-one…
Preparation of (2R, 3S)-3-(benzoylamino)-2-hydroxyphenylpropionic acid ethyl ester_Kain Industrial Additive
Background and overview[1] (2R, 3S)-3-(Benzoylamino)-2-hydroxyphenylpropanoic acid ethyl ester is an important synthetic intermediate that can be used to synthesize the anti-cancer drug paclitaxel. The traditional synthesis method of (2R, 3S)-3-(benzoylamino)-2-hydroxyphenylpropionate ethyl ester mainly involves asymmetric dihydroxylation of α and β unsaturated esters, followed by azide substitution and reduction. be made of. Preparation[1] 1) Add 0.786g…
Preparation of (2R,4S)-5-(biphenyl-4-yl)-4-[(tert-butoxycarbonyl)amino]-2-methylpentanoic acid_Kain Industrial Additive
Background and overview[1] (2R,4S)-5-(biphenyl-4-yl)-4-[(tert-butoxycarbonyl) Amino]-2-methylpentanoic acid is a key intermediate in the preparation of Sacubitril. Sacubitril and valsartan can form the compound drug Entresto at a ratio of 1:1. Entresto is a first-in-class medicine developed by Novartis to reduce the risk of cardiovascular death and hospitalization for heart failure and to reduce ejection fraction in…
