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30484-10-7

7-chloro-2,3,4,5-tetrahydro-1-benzothiepin-5-one synthesis

2synthesis methods
-

Yield:30484-10-7 74.7%

Reaction Conditions:

with polyphosphoric acid for 2 h;

Steps:

5.2 (2) Synthesis of 7-chloro-1-benzothiazepine-one

4-(4-Chlorophenylthio)butyric acid (0.6238 g, 2.70 mmol) and polyphosphoric acid (PPA, 30 g) were weighed into a three-necked flask.After heating at 120 ° C for 2 h with mechanical stirring, the reaction was quenched with ice cubes;The reaction was extracted three times with 25 mL of ethyl acetate.Wash with 5% NaOH and wash with water;The organic layer was taken, dried over anhydrous magnesiumThe T product had a Rf value of 0.658 (TLC, n-hexane-ethyl acetate (95:5)).The crude product is separated by column chromatography and eluted with a developing solvent of n-hexane-ethyl acetate (99:1 to 8:2).The silica gel used had a particle size of 200 to 300 mesh, and the product was obtained in 0.4291 g, and the yield was 74.7%.

References:

CN108640901,2018,A Location in patent:Paragraph 0103; 0109; 0110; 0111