169451-91-6

Upstream product

• 7206-70-4 4-amino-5-chloro-2-methoxybenzoic acid 
• 4023-34-1 cyclopropanecarboxylic acid chloride 
• 20896-27-9 methyl 4-amino-5-chloro-2-methoxybenzoate 
• 1025842-99-2 5-Chloro-4-(cyclopropanecarbonyl-amino)-2-methoxy-benzoic acid methyl ester 

Downstream Products

• 1026950-89-9 5-Chloro-4-(cyclopropanecarbonyl-amino)-2-methoxy-N-[(S)-1-(2,2,2-trifluoro-acetyl)-pyrrolidin-3-yl]-benzamide 
• 224304-78-3 C₁₅H₁₆ClNO₆ 

Relevant academic research and scientific papers

Process for producing 1H-3-aminopyrrolidine and derivatives thereof

A process for producing 1H-3-aminopyrrolidine and derivatives thereof is disclosed. The process is especially useful for producing optically active 1H-3-aminopyrrolidine and derivatives thereof and in this case comprises reacting an optically active amino-protected aspartic anhydride represented by the formula (1) with a primary amine represented by the formula R'NH2, subjecting the reaction product to cyclodehydration to obtain an optically active 1-aralkyl-3-(protected amino)pyrrolidine-2,5-dione compound represented by the formula (2), subsequently eliminating the protective group from the 3-position amino group of the compound represented by the formula (2) to obtain an optically active 1-aralkyl-3-aminopyrrolidine-2,5-dione compound represented by the formula (3), reducing the carbonyl groups of the compound represented by the formula (3) to obtain either an optically active 1-aralkyl-3-aminopyrrolidine compound represented by the formula (4) or a salt thereof with a protonic acid, and then subjecting the compound represented by the formula (4) or the salt thereof to hydrogenolysis to obtain an optically active 1H-3-aminopyrrolidine or a protonic acid salt thereof.

Dopamine D3 and D4 receptor antagonists: synthesis and structure--activity relationships of (S)-(+)-N-(1-Benzyl-3-pyrrolidinyl)-5-chloro-4- [(cyclopropylcarbonyl) amino]-2-methoxybenzamide (YM-43611) and related compounds.

In this study, we synthesized a series of (S)-N-(3-pyrrolidinyl)benzamide derivatives, 1, 2a-d, 5a-1, and 7, and their enantiomers, (R)-1 and (R)-5c-e, and evaluated their binding affinity for cloned dopamine D2, D3, and D4 receptors and their inhibitory