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Synthesis of new aspartic acid analogues incorporating phosphinic acid moiety

Dmitry E Ivanov 1
Dmitry E Ivanov
, 
Alexey Vladimirovich Borodachev 1
Alexey Vladimirovich Borodachev
, 
Maxim Eduardovich Dmitriev 1
Maxim Eduardovich Dmitriev
, 
Valery Vladimirovich Ragulin 1
Valery Vladimirovich Ragulin
10.71267/mencom.8086
Published 23 September 2026
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Ivanov D. E. et al. Synthesis of new aspartic acid analogues incorporating phosphinic acid moiety // Mendeleev Communications. 2026.
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Ivanov D. E., Borodachev A. V., Dmitriev M. E., Ragulin V. V. Synthesis of new aspartic acid analogues incorporating phosphinic acid moiety // Mendeleev Communications. 2026.
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TY - JOUR
DO - 10.71267/mencom.8086
UR - https://mendcomm.colab.ws/publications/10.71267/mencom.8086
TI - Synthesis of new aspartic acid analogues incorporating phosphinic acid moiety
T2 - Mendeleev Communications
AU - Ivanov, Dmitry E
AU - Borodachev, Alexey Vladimirovich
AU - Dmitriev, Maxim Eduardovich
AU - Ragulin, Valery Vladimirovich
PY - 2026
DA - 2026/09/23
PB - Mendeleev Communications
ER -
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@article{2026_Ivanov,
author = {Dmitry E Ivanov and Alexey Vladimirovich Borodachev and Maxim Eduardovich Dmitriev and Valery Vladimirovich Ragulin},
title = {Synthesis of new aspartic acid analogues incorporating phosphinic acid moiety},
journal = {Mendeleev Communications},
year = {2026},
publisher = {Mendeleev Communications},
month = {Sep},
url = {https://mendcomm.colab.ws/publications/10.71267/mencom.8086},
doi = {10.71267/mencom.8086}
}
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Keywords

amidoalkylation
aspartic acid
Kabachnik--Fields reaction
Michael--Pudovik addition
organophosphorus compounds
phosphinic analogues of amino acids
phospholactones
phosphonous carboxylic acids
silylation

Abstract

The synthesis of new aspartic acid analogues incorporating phosphinic acid moiety, promising ligands of MGlu4R receptors, is proposed. The key steps of the synthesis are the Kabachnik–Fields P-functionalization of the P(O)(OH)H group in 2-acetamido-2-carboxyethylphosphonous acid (β-phosphonous isostere of N-acetylaspartic acid), or its Michael–Pudovik addition to acrylates.

Funders

Russian Science Foundation
23-23-00158
Ministry of Education and Science of the Russian Federation
FFSG-2024-0019