Electric Literature of 139481-72-4, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 139481-72-4 name is Trityl candesartan, This compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.
Example 15: Deprotection without Acid; A solution of trityl candesartan c (TCS, 350 g, 410.3 mmol), toluene (1050 mL), methanol (2100 mL) and water (17.0 mL) was refluxed for about 2-4 h (HPLC control), the solvents were evaporated at 40-50 C/P<100 mbar to give a residue as a viscous oil, the residue was dissolved at 45-55 C in a mixture of Toluene/Methanol (1041g, 95: 5, w/w) to give a clear solution. The solution was cooled to (-5)- (20) C the solution was kept at this temperature for about 8-12 hr, the precipitated solids were filtered off, washed on the filter with cold Toluene (350 mL) to give a wet solid (295.8 g, 83.0%) 110 g of the wet solid were dried at 50C/10 mbar for 2-6 hr to give a wet white solid (94g (LOD= 15-25%) ). The wet white solid (43.75 g) was dissolved at 40-60 C in Ethanol Absolute (215-363 mL 6- 10V), the solution was filtered and returned to the reactor, then the solution was cooled to (-15)- (5) C and was kept at this temperature for about 2-24 hr. The precipitated solids were filtered off, washed with cold Ethanol Absolute (23-35 mL) to give wet solid which was dried at 50 C/10 mbar to constant weight to give cilexetil candesartan (21.5 g, 67 %).
At the same time, in my other blogs, there are other synthetic methods of this type of compound, Trityl candesartan, and friends who are interested can also refer to it.
Reference:
Patent; TEVA PHARMACEUTICAL INDUSTRIES LTD.; TEVA PHARMACEUTICALS USA, INC.; WO2005/37821; (2005); A2;,
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