摘要:
The present invention relates to a maleic acid salt of (2S)-N-{5-[amino(imino)methyl]-2-thienyl}methyl-1-{(2R)-2-[(carboxymethyl)amino]-3,3-diphenylpropanoyl}-2-pyrrolidinecarboxamide.
摘要:
The present invention relates to crystalline forms of (2S)-N-5-[amino(imino)methyl]-2-thienyl-methyl-1-(2R)-2-[(carboxymethyl)amino]-3,3-diphenylpropanoyl-2-pyrrolidinecarboxamide nH2O.
摘要:
Disclosed is a process for preparing a compound of the following formula (2): including the steps of reacting a compound of the following formula (4): with trityl chloride to prepare trityloxy-acetic acid ethyl ester of the following formula (8): reacting the compound of formula (8) with ethyl magnesium halide to prepare 1-trityloxymethyl-cyclopropanol of the following formula (9): combining the 1-trityloxymethyl-cyclopropanol of formula (9) with diisopropylbromo-methylphosphonate in a solvent in the presence of a base to prepare (1-trityloxymethyl-cyclopropoxymethyl)-phosphonic acid diisopropyl ester of the following formula (10): as a solid form, and converting the trityl group of the compound of formula (10) into a hydroxyl group.
摘要:
The present invention relates to a new process for preparing diisopropyl {[1-(hydroxymethyl)-cyclopropyl]oxy}methylphosphonate (2), which is a key intermediate for synthesizing an antiviral (particularly, against hepatitis B virus) nucleoside analogue. The present invention also relates to new intermediates, and a process for preparing the antiviral nucleoside analogue from the compound (2) prepared according to the present invention.