تفاعل #66867

معادلة التفاعل

N-(3-chloro-4-fluorophenyl)-5,6,7,8-tetrahydropyrido[4′,3′:4,5]furo[2,3-d]pyrimidin-4-amine

N-(3-Chloro-4-fluorophenyl)-5,6,7,8-tetrahydropyrido[4′,3′:4,5]furo[2,3-d]pyrimidin-4-amine

(2E)-4-(dimethylamino)but-2-enoic acid hydrochloride

(2E)-4-(Dimethylamino)but-2-enoic acid hydrochloride

DIPEA

TBTU

→

title compound

المردود 56.3%

N-(3-Chloro-4-fluorophenyl)-7-[(2E)-4-(dimethylamino)but-2-enoyl]-5,6,7,8-tetrahydropyrido[4′,3′:4,5]furo[2,3-d]pyrimidin-4-amine

المردود 56.3%

المذيبات

THF

ظروف التفاعل

المعالجة

1. 1
   أخرىpurified directly by preparative HPLC
2. 2
   أخرىThe product crystallized upon trituration with diethyl ether

الإجراء التجريبي

A suspension of N-(3-chloro-4-fluorophenyl)-5,6,7,8-tetrahydropyrido[4′,3′:4,5]furo[2,3-d]pyrimidin-4-amine from Example 39A (100 mg, 0.314 mmol) and (2E)-4-(dimethylamino)but-2-enoic acid hydrochloride from Example 1A (73 mg, 0.44 mmol) in THF (2 mL) was treated with DIPEA (160 mg, 1.26 mmol) and TBTU (150 mg, 0.47 mmol). The mixture was stirred at rt overnight and then purified directly by preparative HPLC. The product crystallized upon trituration with diethyl ether to afford 76 mg (56%) of the title compound.

المصدر