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US 8,481,728 B2Granted
Process for preparing entecavir and its intermediates
AssigneeScinoPharm Taiwan, Ltd.
InventorsTsung-Cheng Hu, Hung-Tsung Huang
Life of this patent
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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.
Claims17
A process of making entecavir of the following formula:
- comprising reacting a compound of formula (M5)
- with a compound of formula (A):
- to give a compound of formula (M6):
- and
- de-protecting and/or hydrolyzing the compound of formula (M6) to obtain entecavir,
- wherein the two PGs on the formula (M5) are taken together with the two oxygen atoms to which they attach and the carbon atoms between the two oxygen atoms to form an optionally substituted six- or seven-member ring, R1 on formulae (A) and M6 is halogen;
- R2 and R3 on formulae (A) and M6 are independently defined as H or an amino protecting group.
4 more elements
A process for preparing a compound of formula
- comprising:
- oxidizing a compound of formula (M2):
- to provide an intermediate of formula (IM1):
- and
- hydrolyzing the intermediate of formula (IM1) to the compound of formula (M5);
- wherein the two PGs on the formula (IM1), (M2) and (M5) are taken together with the two oxygen atoms and the carbon atoms between the two oxygen atoms to form an optionally substituted six- or seven-member ring.
3 more elements
A compound of formula (IM1):
- wherein each of the PGs is independently a hydroxy protecting group, or taken together with the two oxygen atoms to which they attach and the carbon atoms between the two oxygen atoms to form an optionally substituted six- or seven-member ring.
A compound with one of the following formulae:
- wherein the two PGs on the formulae (M1), (M2) and (M5) are taken together with the two oxygen atoms to which they attach and the carbon atoms between the two oxygen atoms to form an optionally substituted six- or seven-member ring.
Dependencies are inferred from the claim text.