Title:
イミダゾ［１，２－Ａ］ピリミジンの位置選択的合成
Document Type and Number:
Japanese Patent JP7384926
Kind Code:
B2
Abstract:
A method of regio-selectively synthesizing an imidazo-pyrimidine compound of formulae (XXa) or (XXb)comprising a step of coupling a first compound of formula XX-P1a or XX-P1b with a second compound of formula XX-P2This annulation reaction between β-ethoxy acrylamides and phosphorylated aminoimidazoles to furnish imidazo[1,2-a]pyrimidin-amines relies on steering effects from endocyclic and exocyclic phosphorylated aminoimidazoles. The reaction furnishes either 2-amino or 4-amino constitutional isomers of imidazo[1,2-a]pyrimidines with good yields and ranges of 90:10-99:1 regio-selectivity. The reaction is useful in the synthesis of various tracer molecules used in the study of neurological conditions such as where R3 and R4 together with the imidazole ring atoms to which they are bonded form a phenyl ring and the products are substituted benzimidazopyrimidines. The reaction can be generalized to form imidazo[1,2-a]pyrimidines substituted at either of their 2- and 4-positions by alkoxy or thioalkyl groups.
Inventors:
Crag, Kyle Bradley Pascal
White, Nicholas Andrew
Chan, Haimin
Goslan, Francis
Nack, William
O'Shea, Paul Dee.
White, Nicholas Andrew
Chan, Haimin
Goslan, Francis
Nack, William
O'Shea, Paul Dee.
Application Number:
JP2021566476A
Publication Date:
November 21, 2023
Filing Date:
May 07, 2020
Export Citation:
Assignee:
Ef Hoffman-La Roche Akchengezel Shaft
International Classes:
C07D487/04
Domestic Patent References:
| JP2013522365A |
Foreign References:
| US3111525 |
Other References:
Bioorganic & Medicinal Chemistry Letters,2014年,24(1),P.254-257
Attorney, Agent or Firm:
Sonoda & Kobayashi Patent Attorneys Corporation
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