Procedure for the preparation of 3 alphaphosphate 11-oxo 2,20-bis-hydroxymethyl 5 betapregnan and its alkaline salts (Machine-translation by Google Translate, not legally binding)

摘要

Process for the preparation of 3-alpha-phosphate 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane of the formula: ** (See formula) ** and its alkali metal salts, especially the disodium salt of 3-alpha-phosphate 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane, as well as, of its mineral or organic esters on the hydroxymethyl groups in 20, especially 3-alpha-phosphate. -oxo-20,20-bis-nitratomethyl-5-beta-pregnane, mainly characterized in that; the acetonide of 3alpha-hydroxy 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane is subjected to the action of a functional derivative of phosphoric acid, such as a dibenzyl halogen-phosphonate, obtaining, in this case, the 3alpha - corresponding pregnane diphenyl phosphate; - the 20,20-bis-hydroxymethyl functions of the obtained 3alpha-dibenzylphosphate 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane acetonide are unblocked, obtaining 3alpha-dibenzylphosphate 11-oxo 20,20-bis-liydroxymethyl 5beta Pregnane; - the dibenzylphosphate group is subjected to hydrogenolysis in 3 of the compound whose 20,20-bis-hydroxymethyl-5-beta-pregnane functions have been released, obtaining the 3-alpha-phosphate 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane, which, if necessary, it can be converted into an alkaline salt, such as the 3alpha-phosphate 11-oxo-20,20-bis-hydroxymethyl-5-beta-pregnane disodium salt, or in a mineral or organic ester, such as 3-phosphate-3-phosphate. -oxo 20,20-bis-nitratomethyl 5beta-pregnane. (Machine-translation by Google Translate, not legally binding)