4-acetyl-6-chloro-3-(isopropylamino)-2H-thieno[2,3-e][1,2,4]thiadiazine-1,1(4H)-dione -Drug Synthesis Database

【结构式】

【分子编号】51339

【品名】4-acetyl-6-chloro-3-(isopropylamino)-2H-thieno[2,3-e][1,2,4]thiadiazine-1,1(4H)-dione

【CA登记号】

【分子式】C₁₀H₁₂ClN₃O₃S₂

【分子量】321.8084

【元素组成】C 37.32% H 3.76% Cl 11.02% N 13.06% O 14.92% S 19.93%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号：(III)

The thiocarbamoylation of the thiophenesulfonamide (I) with isopropyl isothiocyanate in the presence of potassium tert-butoxide furnished the sulfonyl thiourea (II). This was cyclized to the thienothiadiazine derivative (III) upon treatment with phosgene and triethylamine in cold THF. The acetyl group of (III) was finally removed by hydrolysis with NaOH.

参考文献中间体

合成目标

【1】 Tagmose, T.M.; Hansen, H.C.; Nielsen, F.E.; Mogensen, J.P.; Hansen, J.B. (Novo Nordisk A/S); Fused 1,2,4-thiadiazine derivs., their preparation and use. EP 1000066; JP 2001510195; WO 9903861 .

中间体序号	中间体编号	品名	分子式	供应商	用于合成
(I)	51337	N-[3-(aminosulfonyl)-5-chloro-2-thienyl]acetamide	C₆H₇ClN₂O₃S₂	详情	详情
(II)	51338	N-[5-chloro-3-([[(isopropylamino)carbothioyl]amino]sulfonyl)-2-thienyl]acetamide	C₁₀H₁₄ClN₃O₃S₃	详情	详情
(III)	51339	4-acetyl-6-chloro-3-(isopropylamino)-2H-thieno[2,3-e][1,2,4]thiadiazine-1,1(4H)-dione	C₁₀H₁₂ClN₃O₃S₂	详情	详情

Extended Information