A highly enantioselective synthetic method towards the α2c-adrenoceptor antagonist ORM-10921-Reference-Cited by-同舟云学术

A highly enantioselective synthetic method towards the α2c-adrenoceptor antagonist ORM-10921

Published:2019 Issue:6 Volume:6 Page:773-779
ISSN:2052-4129
Container-title:Organic Chemistry Frontiers
language:en
Short-container-title:Org. Chem. Front.

Author:

Ma Qiaoning¹²³⁴,Yang Xiaodi⁵⁶⁷⁴,Lei Xinsheng¹²³⁴^ORCID,Lin Guo-Qiang¹²³⁴⁵

Affiliation:

1. Institutes of Biomedical Sciences & School of Pharmacy

2. Fudan University

3. Shanghai 201203

4. China

5. Experiment Center for Science and Technology

6. Shanghai University of Traditional Chinese Medicine

7. Shanghai

Abstract

The preparation of ORM-10921, a selective α_2C-adrenoceptor antagonist with promising anti-psychotic properties, was successfully achieved using asymmetric α-alkylation of α,β-unsaturated imide and Bischler–Napieralski cyclization/asymmetric reduction as the key steps.

Funder

National Natural Science Foundation of China

Publisher

Royal Society of Chemistry (RSC)

Subject

Organic Chemistry

Link

http://pubs.rsc.org/en/content/articlepdf/2019/QO/C8QO01166D

Reference31 articles.

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2. Cognitive dysfunction in psychiatric disorders: characteristics, causes and the quest for improved therapy

3. Structure–function prediction of α2A-, α2B-, and α2C-adrenoceptors using homology model assisted antagonist binding study

4. Therapeutic Potential of Selectively Targeting the α2C-Adrenoceptor in Cognition, Depression, and Schizophrenia—New Developments and Future Perspective

5. α2-Adrenoceptor Antagonists: Synthesis, Pharmacological Evaluation, and Molecular Modeling Investigation of Pyridinoguanidine, Pyridino-2-aminoimidazoline and Their Derivatives

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1. Synthesis, biological evaluation, and molecular modeling of ORM‐10921 and its analogs as α_2C‐adrenoceptor antagonists;Archiv der Pharmazie;2023-05-18