- Synthetic method of (R)-(1-amino-3-methyl)butyl-1-pinane borate terephthalate
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The invention discloses a synthetic method of (R)-(1-amino-3-methyl) butyl-1-pinane borate terephthalate (The formula I). The synthetic method is characterized in that (R)-1-amino-3-methyl butane-1-boronic acid pinacol ester hydrochloride is taken as a raw material, and a target product is obtained by amino protection, boron ester exchange and deprotection. The method disclosed by the invention has the advantages of fewer reaction steps, mild reaction conditions, low price of used reagents, high purity of products and the like; in addition, the industrial production is facilitated.
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Paragraph 0053; 0058; 0063; 0064; 0072
(2018/05/16)
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- Preparation of (1R)-(S)-pinane diol-1-amino-3-methyl-butane-1-borate and a salt thereof
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The invention discloses a method for preparing (1R)-(S)-pinanediol-1-amino-3-methylbutane-1-borate ester and a salt thereof. The method for preparing (1R)-(S)-pinanediol-1-amino-3-methylbutane-1-borate ester comprises step A and step B in the following synthetic route, wherein in the formula, X represents a halogen atom and M represents an alkali metal. (1R)-(S)-pinanediol-1-amino-3-methylbutane-1-borate ester is subjected to a salt forming reaction with an organic acid or an inorganic aid, and an acidic salt of (1R)-(S)-pinanediol-1-amino-3-methylbutane-1-borate ester is obtained. The method of the invention can help to synthesize high-purity bortezomib or other boropeptide compounds in low cost, is accord with industrial production requirements and has practical value.
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