Triethylamine → 4(5-Phenylmethylthio-7-chloro-thiazolo[4,5-d]pyrimidin-2-ylamino)-piperidine-1-carboxylic acid tert-butyl ester

関与物質

役割	名称	HCID	仕込み量
反応物	Triethylamine	HCID 8471	—
反応物	4-Amino-1-Boc-piperidine	HCID 1268291	—
反応物	5-(Benzylthio)-2-bromo-7-chlorothiazolo[4,5-d]pyrimidine	HCID 22052038	—
溶媒	Acetonitrile	HCID 6342	—
生成物	4(5-Phenylmethylthio-7-chloro-thiazolo[4,5-d]pyrimidin-2-ylamino)-piperidine-1-carboxylic acid tert-butyl ester	HCID 86760110	57.5%

反応条件

温度	35 °C

反応手順

5-Phenylmethylthio-2-bromo-7-chloro-thiazolo[4,5-d]pyrimidine (WO 00/09511) (525 mg, 1.4 mmol), 4-amino-1-N-Boc-piperidine (339 mg, 1.7 mmol) and triethylamine (196 μL, 1.4 mmol) were dissolved in anhydrous acetonitrile (15 mL) and the mixture was stirred under a nitrogen atmosphere at 35° C. for 24 hours. The mixture was filtered and the remaining solid was washed with acetonitrile. After drying in air for 48 hours, 396 mg (57% yield) of the title compound was obtained as a white solid.

情報源と証拠

DOI	10.6084/m9.figshare.5104873.v1
特許番号	US07067657B2
出典データセット	uspto-grants-2006_06
ORD ID	ord-9eec80bca90e411aae41bd6949dce338
出典メモ	uspto-grants-2006_06