تفاعل #1340620

معادلة التفاعل

ethyl 2-(4,4-difluoropiperidin-1-yl)benzo[d]thiazole-6-carboxylate

ethyl 2-bromo-benzo[d]thiazole-6-carboxylate

4,4-difluoropiperidine

Cs2CO3

HCl

→

49d

المردود 99.0%

2-(4,4-Difluoropiperidin-1-yl)benzo[d]thiazole-6-carboxylic acid

المردود 99.0%

المذيبات

water

CH3CN

ظروف التفاعل

المعالجة

1. 1
   درجة الحرارةwas refluxed overnight
2. 2
   درجة الحرارةThe reaction mixture was heated at 60° C. for 18 h
3. 3
   درجة الحرارةAfter cooling
4. 4
   ترشيحthe resulting precipitate was filtered

الإجراء التجريبي

A mixture of ethyl 2-bromo-benzo[d]thiazole-6-carboxylate 49a (1.75 mmol, 500 mg), 4,4-difluoropiperidine 49b (1.92 mmol, 303 mg), and Cs2CO3 (5.24 mmol, 1.71 g) in 15 mL of CH3CN was refluxed overnight. The suspension was cooled to room temperature and 15 mL of water was added to the mixture (containing ethyl 2-(4,4-difluoropiperidin-1-yl)benzo[d]thiazole-6-carboxylate 49c). The reaction mixture was heated at 60° C. for 18 h. After cooling, the mixture was acidified using 3N aqueous HCl and the resulting precipitate was filtered to give 575 mg (99%) of 49d. MS m/z (M+H+) 299.1.

المصدر