3,5-dichloroisothiazole-4-carbonitrile synthesis

Yield:-

Reaction Conditions:

with chlorine in tetrachloromethane at 25; for 4 h;Inert atmosphere;

Steps:

135.2 Step 2: Dichloro-1,2-thiazole-4-carbonitrile
Step 2: Dichloro-1,2-thiazole-4-carbonitrile [1011] [1012] Into a 500-mL 3-necked round-bottom flask purged and maintained with an inert atmosphere of nitrogen, was placed a solution of 2-(2,4-dithia-1,5-disodapentan-3-ylidene)propanedinitrile (40 g, 214.86 mmol, 1.00 equiv) in CCl₄ (300 mL). To the above Cl₂(g) was introduced in. The resulting solution was stirred for 4 h at 25° C. The solids were filtered out, washed with 3×50 mL of DCM. The DCM phase were combined and concentrated. This resulted in 3.5 g (crude) of dichloro-1,2-thiazole-4-carbonitrile as brown oil.

References:

Janssen Pharmaceutica NV;Sui, Zhihua;Cai, Chaozhong;Zhang, Xuqing US2014/275179, 2014, A1 Location in patent:Paragraph 1011; 1012

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