Fronepidil synthesis

Yield:-

Reaction Conditions:

with sodium hydroxide in water;

Steps:

2 1-(1-methyl-1-phenyl-2-propynyloxy)-2-(N-pyrrolidinyl)-3-isobutoxy propane

EXAMPLE 2 1-(1-methyl-1-phenyl-2-propynyloxy)-2-(N-pyrrolidinyl)-3-isobutoxy propane In a corresponding manner as described in the previous example 6 g of the liquid product of the heading were obtained by refluxing for 5 hours a mixture constituted by 14.6 g of 2-phenyl-3-butyne-2-ol, 10 g of sodium hydroxide in 10 ml of water, 1,1 g of benzyl triethylammonium chloride and 11 g of 1-pyrrolidinyl-2-chloro-3-isobutoxy propane. BP₀,5 =143°-145° C.; n_D²⁰ =1.502. The liquid base thus obtained was converted into the hydrochloride salt. Melting point HCl salt: 154° C. Elemental analysis:

References:

US4430332,1984,A