O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate → (6-Chloro-pyrazolo[1,5-a]pyrimidin-2-yl)-(2-methyl-4,5,7,8-tetrahydro-thiazolo[4,5-d]azepin-6-yl)-methanone

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Reaction Steps

0.72 g (2.23 mmol) TBTU was added to 0.40 g (2.03 mmol) 6-Chloro-pyrazolo[1,5-a]pyrimidine-2-carboxylic acid, 0.41 g (2.03 mmol) 2-Methyl-5,6,7,8-tetrahydro-4H-thiazolo[4,5-d]azepine hydrochloride and 0.88 mL (6.28 mmol) TEA in 8.0 mL DMF and stirred at RT overnight. The reaction mixture was purified by HPLC chromatography and lyophilized. Yield: 0.18 g (25% of theory). ESI-MS: m/z=348 (M+H)+; Rt(HPLC): 1.01 min. (Method J).

Provenance & Evidence