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US 10,865,212 B2Granted
Intermediate for preparing eribulin mesylate and process for preparing the same
AssigneeYonsung Fine Chemical Co., Ltd.
InventorsHyoseon Lee, Hyunik Shin, Keeyoung Lee, Changyoung Oh
Life of this patent
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Abstract
The present invention relates to a process for preparing an intermediate for the preparation of eribulin mesylate with high yields, and an intermediate therefor.
Claims9
A process for preparing a compound of the following formula (3), which comprises the steps of:
- subjecting a compound of the following formula (4) to Wittig reaction to obtain a compound of the following formula (5);
- (ii) selectively deprotecting a PG2 group of the compound of the following formula (5) to obtain a compound of the following formula (6);
- (iii) subjecting the compound of the following formula (6) to cyclization to obtain a compound of the following formula (7);
- (iv) subjecting the compound of the following formula (7) to hydrogenation to obtain a compound of the following formula (8);
- and
- (v) reducing an ester group of the compound of the following formula (8):
- wherein,
- PG1 represents a diol protecting group forming a 5-membered heterocycle by combining each other, and is derived from cyclopentanone, cyclohexanone, cycloheptanone, 1,1-dimethoxycyclopentane, 1,1-dimethoxycyclohexane or 1,1-dimethoxycycloheptane,
- PG2 represents a silyl protecting group, and
- R1 represents hydrogen or a C1-C6 alkyl group.
7 more elements
A compound of the following formula (3):
- wherein,
- PG1 represents a diol protecting group forming a 5-membered heterocycle by combining each other, and is derived from cyclopentanone, cyclohexanone, cycloheptanone, 1,1-dimethoxycyclopentane, 1,1-dimethoxycyclohexane or 1,1-dimethoxycycloheptane.
Dependencies are inferred from the claim text.