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1-(DIPHENYLMETHYL)-3-METHYL-3-AZETIDINAMINE synthesis

2synthesis methods
-

Yield:133891-52-8 98%

Reaction Conditions:

with ammonia in methanol at 20; for 20 h;

Steps:

41.iii

To a solution of ammonia (100ml, 7N in methanol) was added methanesulfonic acid l-benzhydryl-3-methyl-azetidin-3-yl ester (5.2g, 15.8mmol) and the reaction stirred at r.t. for 20 hours. The solution was evaporated in vacuo and the residue was purified by flash chromatography eluting with Methanol/DCM (1 : 10) to afford the title compound as a white foam. Yield 3.9g (98 %): HPLC retention time, 3.40min (Solvent: CH3CN/H2O/0.05% NH3, 5-95% gradient H2O-6min. Column: Xterra 50 x EPO 4.60 i.d., Cl 8 reverse phase. Flow rate: 1.5mL/min.). Mass spectrum (ES+) m/z 253 (M + H).

References:

WO2007/7057,2007,A1 Location in patent:Page/Page column 35-36

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