Cyclopropylboronic acid → 1-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine hydrochloride

HRID 1804023Notes

Reaction equation

HRID 1804023 reaction equation
C(OC([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[C:19]([Cl:20])=[CH:18][C:17]([C:21]([F:24])([F:23])[F:22])=[CH:16][N:15]=2)[CH2:10][CH2:9]1)=O)(C)(C)C.[CH:25]1(B(O)O)[CH2:27][CH2:26]1>>[ClH:20].[CH:25]1([C:19]2[C:14]([N:11]3[CH2:10][CH2:9][NH:8][CH2:13][CH2:12]3)=[N:15][CH:16]=[C:17]([C:21]([F:22])([F:23])[F:24])[CH:18]=2)[CH2:27][CH2:26]1

Participants

3

Reactant 2

HCID 2760897Cyclopropylboronic acidHCID 573664161-Tert-butyloxycarbonyl-4-(3-chloro-5-(trifluoromethyl)pyridin-2-YL)piperazine

Product 1

HCID 673807791-(3-Cyclopropyl-5-trifluoromethylpyridin-2-yl)piperazine hydrochlorideYield 94.4%

Procedure

By reaction and treatment in the same manner as in Preparation Example 49 and using 4-(3-chloro-5-trifluoromethylpyridin-2-yl)piperazine-1-carboxylic acid tert-butyl ester (7.3 g), which is the intermediate described in Preparation Example 51, and cyclopropylboronic acid (4.2 g), the title compound (5.8 g) was obtained.

Workup

  1. customBy reaction and treatment in the same manner
  2. customas in Preparation Example 49

Sources & evidence

ORD record
ord-2fe81650481245789a299cf27e8a016c
Source dataset
uspto-grants-2013_01
Patent number
US08354401B2

Reaction notes

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