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US 10,851,100 B2Granted
Preparation method for and intermediate of pyrrolo six-membered heteroaromatic ring derivative
AssigneeJiangsu Hengrui Medicine Co., Ltd.
InventorsBing Liu, Lin Bian, Xiaohui Gao
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Abstract
Disclosed are an intermediate of a pyrrolo six-membered heteroaromatic ring derivative as a JAK inhibitor and a preparation method therefor, and a method for preparing a pyrrolo six-membered heteroaromatic ring derivative using the intermediate. The method improves the reaction yield, is simple and easy to operate and control, and is conducive to expanded industrial production.
Claims12
A compound of formula (I) or a stereoisomer thereof:
- wherein,
- R1 is hydrogen or an amino protecting group;
- R2 is an amino protecting group;
- R3 is selected from the group consisting of hydrogen, C1-6 alkyl and an amino protecting group;
- the amino protecting group is selected from the group consisting of alkoxycarbonyl amino protecting group, acyl amino protecting group, sulfonyl amino protecting group, and alkyl amino protecting group;
- the alkoxycarbonyl amino protecting group is selected from the group consisting of benzyloxycarbonyl, tert-butoxycarbonyl, fluorenylmethoxycarbonyl, allyloxycarbonyl, trimethylsilylethoxycarbonyl, methoxycarbonyl, and ethoxycarbonyl;
- the acyl amino protecting group is selected from the group consisting of phthalyl, trifluoroacetyl, pivaloyl, benzoyl, formyl, and acetyl;
- the sulfonyl amino protecting group is selected from the group consisting of p-toluenesulfonyl, o-nitrobenzenesulfonyl, and p-nitrobenzenesulfonyl;
- and
- the alkyl amino protecting group is selected from the group consisting of trityl, 2,4-dimethoxybenzyl, p-methoxybenzyl, and benzyl.
7 more elements
Dependencies are inferred from the claim text.