Process for preparing chiral dipeptidyl peptidase-IV inhibitors

US10053466B2 · US · B2

Patent metadata
FieldValue
Publication numberUS-10053466-B2
Application numberUS-201715831895-A
CountryUS
Kind codeB2
Filing dateDec 5, 2017
Priority dateJul 21, 2014
Publication dateAug 21, 2018
Grant dateAug 21, 2018

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  1. Title

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  2. Abstract

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  3. Assignees and inventors

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  4. Key dates

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  5. First independent claim

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  6. CPC / IPC classifications

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  7. Citations and related patents

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Abstract

Official abstract text for this publication.

A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of:  and reductive amination of:

First claim

Opening claim text (preview).

What is claimed is: 1. A process of preparing a compound of Formula 7 comprising reacting 2,4-difluorobenzaldehyde and nitromethane in the present of a copper salt, ligand, base and solvent to produce a compound of Formula 17: 2. The process of claim 1 further comprising the step of reacting the compound of Formula 17 with acrolein in the presence of a base and solvent to produce a compound of Formula 18: 3. The process of claim 2 further comprising the step of reacting the compound of Formula 18 with a chlorinating agent in the presence of a base and a solvent to produce a compound of Formula 19: 4. The process of claim 3 further comprising the step of crystallizing the compound of Formula 19 under basic conditions to produce a compound of Formula 19t: 5. The process of claim 4 further comprising the steps of reacting the compound of Formula 19t with a hydrobrating agent and an oxidant to produce a compound of Formula 20: and reacting the compound of Formula 20 with a reducing agent and a protecting group to produce a compound of Formula 21:

Assignees

Inventors

Classifications

  • Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

  • condensed with heterocyclic ring systems · CPC title

  • C07D487/04Primary

    Ortho-condensed systems · CPC title

  • Oxygen atoms, e.g. delta-lactones · CPC title

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Frequently asked questions

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What does patent US10053466B2 cover?
A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of:  and …
Who is the assignee on this patent?
Merck Sharp & Dohme
What technology area does this patent fall under?
Primary CPC classification C07D487/04. Mapped technology areas include Chemistry & Metallurgy.
When was this patent published?
Publication date Tue Aug 21 2018 00:00:00 GMT+0000 (Coordinated Universal Time) (B2). Legal status and post-grant events are not shown on this page.
What related patents are in patentsdb?
We list 1 related publication on this page (citations in our corpus or others sharing the same primary CPC).