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US 10,766,900 B2Granted
Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
AssigneeFormosa Laboratories, Inc.
InventorHsiang-Yun Lai
Life of this patent
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Abstract
The present disclosure provides a Baricitinib intermediate, a method for preparing the Baricitinib intermediate, and a method for preparing Baricitinib or a pharmaceutically acceptable salt thereof using the Baricitinib intermediate. The method for preparing the Baricitinib intermediate involves the use of a divalent palladium catalyst or a nickel catalyst and provides the Baricitinib intermediate in high yield.
Claims12
A method for forming a compound of formula (1):
- wherein R1 is CH2OC(O)R′, R′ is a substituted or unsubstituted alkyl group or a substituted or unsubstituted cycloalkyl group, and R2 is selected from the group consisting of substituted or unsubstituted cyclic ether group, 1-(ethoxy)ethyl group, p-methoxybenzyl group, triphenylmethyl group, diphenylmethyl group, hydroxymethyl group, methoxymethyl group, triisopropylsilyl group and t-butyldimethylsilylmethyl group, comprising:
- reacting a compound of formula (2) with a boron-containing compound selected from the group consisting of a compound of formula (3), a compound of formula (4) and a compound of formula (5) in the presence of bis(triphenylphosphine)palladium(II) dichloride (Pd(PPh3)2Cl2) and in the absence of an additional phosphine ligand, wherein the formula (2), the formula (3), the formula (4), and the formula (5) are as follows:
- wherein X is selected from the group consisting of Br, Cl, and I;
- and R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13 and R14 are each independently H or C1-C4 alkyl group.
1 more element
Dependencies are inferred from the claim text.