With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.37441-50-2,1,2-Thiazinane 1,1-dioxide,as a common compound, the synthetic route is as follows.
solution of 2-(3-chloro-4-fluorobenzyl)-8-ethyl-4-fluoro-10-methoxy-6-methyl-7,8- dihydropyrazino[l’,2′: 1,5]pyrrolo[2,3-d]pyridazine-1,9(2H,6H)-dione (0.10 g, 0.23 mmol; Example 139), 1,2-thiazinane 1,1-dioxide (45 mg, 0.33 mmol), and cesium carbonate (0.15 g, 0.46 mmol) in anhydrous DMSO (9.5 mL) was heated in an oil bath at 50 C for 5 hours. The product mixture was filtered through a pad of Celite and the filtrate was subjected to purification on reverse phase preparative HPLC purification. Collection and lyophilization of appropriate fractions afforded the title material. Analytical HPLC indicated that the product is a 1:1 mixture of two isomers that arose from the relative stereochemistry of the 6-methyl group and restricted rotation between the sultam ring and the tricyclic core. ?H NMR (400 MHz, CDCI3) No. 7.48 (m 1H), 7.28 (m, 1H), 7.11 (t, J = 8.5 Hz, 1H), 5.17 (d, J = 14.2 Hz, ?H), 5.34 (in, 1/2 H), 5.29 (d, J = 14.2 Hz, (at)H), 5.23 (d, J = 14.2 Hz, ?H), 5.09 (d, J = 14.2 Hz, ?H), 5.07 (m, ?H), 4.18 (s, 1.5H), 4.16 (s, 1.5H), 4.12-3.17 (m), 2.58-2.00 (m), 1.57 (d, J = 6.6 Hz, 1.5H), 1.42 (d, J = 6.8 Hz, 1.5H), 1.23 (t, J = 6.8 Hz, 1.5H), 1.22 (t, J = 7.1 Hz, 1.5H). ES MS M+1 = 552
37441-50-2 1,2-Thiazinane 1,1-dioxide 303508, athiazines compound, is more and more widely used in various.
Reference£º
Patent; MERCK & CO., INC.; WO2005/110414; (2005); A2;,
Thiazine – an overview | ScienceDirect Topics
Thiazine | C4H5NS – PubChem