Sustainable and Safe N-alkylation of N-heterocycles by Propylene Carbonate under Neat Reaction Conditions

被引：0

作者：

Czompa, Andrea ^{[1
]}

Bogdan, Dora ^{[1
,2
]}

Balogh, Balazs ^{[1
]}

Erdei, Eszter ^{[1
,2
]}

Selymes, Patrik ^{[1
]}

Csomos, Attila ^{[3
,4
]}

Mandity, Istvan M. ^{[1
,2
]}

机构：

[1] Semmelweis Univ, Inst Organ Chem, Hogyes Endre Utca 7, H-1092 Budapest, Hungary

[2] Res Ctr Nat Sci, Inst Mat & Environm Chem, HUN REN Artificial Transporters Res Grp, Magyar Tudosok Korutja 2, H-1117 Budapest, Hungary

[3] Femtonics Ltd, Tuzolto Utca 59, H-1094 Budapest, Hungary

[4] Eotvos Lorand Univ, Hevesy Gyorgy PhD Sch Chem, Pazmany Peter Setany 1-A, H-1117 Budapest, Hungary

来源：

INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES | 2024年 / 25卷 / 10期

关键词：

propylene carbonate; N-alkylation; heterocycles; neat conditions; green chemistry; DENSITY-FUNCTIONAL THEORY; EFFICIENT SYNTHESIS; PK(A) PREDICTION; AMINES;

D O I：

10.3390/ijms25105523

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A new, eco-friendly process utilising the green solvent propylene carbonate (PC) has been developed to perform N-alkylation of N-, O- and/or S-containing heterocyclic compounds. PC in these reactions served as both the reagent and solvent. Importantly, no genotoxic alkyl halides were required. No auxiliary was necessary when using anhydrous PC. Product formation includes nucleophilic substitution with the concomitant loss of water and carbon dioxide. Substrates prepared, including the newly invented PROTAC drugs, are widely used.

引用

页数：14

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