Application of 959992-62-2, These common heterocyclic compound, 959992-62-2, name is 6-Bromo-3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazine, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Example 1173-((3,4-Dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-yl)ethynyl)-7,7-dimethyl-7,8- dihydroquinolin-5(6H)-one[00323]The synthesis of 6-bromo-3,4-dihydro-2/-/-pyrido[3,2-b][1 ,4]oxazine is described in literature (e.g., WO 2007/141473).[00324]A mixture of 6-bromo-3,4-dihydro-2/-/-pyrido[3,2-b][1 ,4]oxazine (107 mg, 0.50 mmol), PdCI2[PPh3]2 (35 mg, 0.05 mmol), and Cul (10 mg, 0.05 mmol) in anhydrous acetonitrile (5 mL) is degassed. Then 3-ethynyl-7,7-dimethyl-7,8-dihydroquinolin-5(6/-/)- one (100 mg, 0.50 mmol) is added followed by TEA (1 mL). The reaction mixture is stirred under argon atmosphere at 60 C for 8 h, cooled down to r.t. and concentrated at reduced pressure. The obtained residue is purified by preparative HPLC (C18, acetonitrile/water) to provide the title compound (32 mg, 20%).1H NMR (CDCI3), deltaEta, 1 .12 (s, 6H), 2.56 (s, 2H), 3.05 (s, 2H), 3.58 (t, 2H), 4.26 (t, 2H), 5.07 (br s, 1 H), 6.89 (d, 1 H), 6.96 (d, 1 H), 8.38 (s, 1 H), 8.84 (s, 1 H).LC/MS (M+H)+ = 334, 375
The synthetic route of 959992-62-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MERZ PHARMA GMBH & CO. KGAA; HENRICH, Markus; ABEL, Ulrich; MULLER, Sibylle; KUBAS, Holger; MEYER, Udo; HECHENBERGER, Mirko; KAUSS, Valerjans; ZEMRIBO, Ronalds; WO2012/52451; (2012); A1;,
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