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US 12,729,212 B2Granted
Method for producing (2-methylpyrimidin-5-yl)boronic acid derivative
AssigneeKaneka Corporation
InventorsYoshinori Hirai, Kohei Mori, Hiroaki Yasukouchi
Life of this patent
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Abstract
A method for producing a (2-methylpyrimidin-5-yl)boronic acid derivative (3) includes the step of decarboxylating a 5-bromopyrimidine derivative (1) to synthesize 5-bromo-2-methylpyrimidine (2). The method enables efficient production of 5-bromo-2-methylpyrimidine (2) with less environmental impact, leading to efficient production of (2-methylpyrimidin-5-yl)boronic acid derivative (3) which is useful as a pharmaceutical intermediate.
Claims7
A method for producing a (2-methylpyrimidin-5-yl)boronic acid derivative represented by the following Formula (3):
- wherein R2 and R3 each independently represent a hydrogen atom or a C1-6 alkyl group optionally having a substituent, and R2 and R3 may be combined to form a ring,
- the method comprising the steps of:
- decarboxylating a 5-bromopyrimidine derivative represented by the following Formula (1):
- wherein R1 represents a hydrogen atom or CO2H,
- to synthesize a 5-bromo-2-methylpyrimidine represented by the following Formula (2):
- ;
- and
- bringing the 5-bromo-2-methylpyrimidine, a trialkoxyboron compound, and an organolithium reagent into contact in a flow reactor, thereby producing the (2-methylpyrimidin-5-yl)boronic acid derivative.
5 more elements
Dependencies are inferred from the claim text.