Back to results
US 2011/0201809 A1Published application
Process for Preparing Entecavir and its Intermediates
AssigneeScinoPharm Taiwan, Ltd.
InventorsTsung-Cheng Hu, Hung-Tsung Huang
Life of this patent
Estimating the term…
Abstract
A process of making entecavir comprising converting a compound of formula (M5) to entecavir, wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.
Claims23
A process of making entecavir of the following formula:
- comprising converting a compound of formula (M5)
- to entecavir,
- wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring.
A process for preparing a compound of formula
- comprising:
- oxidizing a compound of formula (2):
- to provide an intermediate of formula (IM2):
- and
- converting the intermediate of formula (IM2) to the compound of formula (5);
- wherein R1 and R2 each is independently a hydroxy protecting group;
- or R1 and R2 are taken together to form am optionally substituted six or seven member cyclic ring;
- n is 1 to 3.
5 more elements
A compound of formula (IM1):
- wherein each of the PGs is independently a hydroxy protecting group, or taken together to form an optionally substituted six- or seven-member cyclic ring.
A compound with one of the following formulae:
- wherein the two PGs on the formula (M5) are taken together to form an optionally substituted six- or seven-member cyclic ring, or each of the PGs on the formula (M1), (M2) and (M5) independently represents a hydroxyl protecting group selected from the group consisting of tart-butyldimethylsilyl and optionally substituted triphenylmethyl, alkoxymethyl, and arylalkoxymethyl.
Dependencies are inferred from the claim text.