65950-13-2

Upstream product

• 98-88-4 benzoyl chloride 
• 55-21-0 benzamide 
• 23356-96-9 (S)-1-Pyrrolidin-2-yl-methanol 
• 56439-58-8 N,O-Dibenzoyl-L-prolinol 
• 2577-48-2 methyl (2S)-pyrrolidine carboxylate 
• 147-85-3 L-proline 
• 72351-42-9 [2-(hydroxymethyl)-1-pyrrolidinyl](phenyl)methanone 
• 5493-38-9 N-benzoyl-L-proline methyl ester 

Downstream Products

• 106865-54-7 N-benzoyl-L-2<(methylthio)methyl>pyrrolidine 
• 106865-53-6 N-benzoyl-L-(+)-2-<(phenylthio)methyl>pyrrolidine 
• 2315-68-6 propyl benzoate 
• 136-60-7 benzoic acid, butyl ester 
• 478385-97-6 (2S)-1-benzoyl-2-fluoromethylpyrrolidine 
• 65950-14-3 (2S)-1-benzoylpyrrolidin-2-al 

Relevant academic research and scientific papers

Chemoselective Intramolecular Formal Insertion Reaction of Rh–Nitrenes into an Amide Bond Over C?H Insertion

The past few decades have witnessed extensive efforts to disclose the unique reactivity of metal–nitrenes, because they could be a powerful synthetic tool for introducing the amine functionality into unactivated chemical bonds. The reactivity of metal–nitrenes, however, is currently mainly confined to aziridination (an insertion into a C=C bond) and C?H amination (an insertion into a C?H bond). Nitrene insertion into an amide C?N bond, however, has not been reported so far. In this work we have developed a rhodium-catalyzed one-nitrogen insertion into amide C?N and sulfonamide S?N bonds. Experimental and theoretical analyses based on density functional theory indicate that the formal amide insertion proceeds via a rhodium-coordinated ammonium ylide formed between the nitrene and the amide nitrogen, followed by acyl group transfer concomitant with C?N bond cleavage. Mechanistic studies have allowed rationalization of the origin of the chemoselectivity observed between the C?H and amide insertion reactions. The methodology presented herein is the first example of an insertion of nitrene into amide bonds and provides facile access to unique diazacyclic systems with an N?N bond linkage.

Mesoporous niobium oxide spheres as an effective catalyst for the transamidation of primary amides with amines

Mesoporous niobium oxide spheres (MNOS), conveniently prepared by a novel antisolvent precipitation approach, have been shown to be an effective catalyst for the transamidation of primary amides with amines. This novel transamidation can be efficiently carried out under solvent-free conditions and is applicable to a wide range of primary amides and amines to provide N-alkyl amides in good to excellent yields. The catalyst is highly stable and reusable. The application of this transamidation reaction has been demonstrated in the synthesis of antidepressant drug moclobemide and other druglike compounds.

Simple methodology for the preparation of amino alcohols from amino acid esters using nabh4-methanol in THF

Amino alcohols constitute a very useful and versatile class of organic compounds, with important applications in synthetic and medicinal chemistry. However, in most of the procedures described in the literature for the obtainment of these compounds, considerable limitations can be found, such as drastic conditions, long time reactions, poor yields, and purification problems. The present article describes a methodology that gives amino alcohols and N-protected amino alcohols based on the reduction of amino acid esters under mild conditions, employing NaBH4 in the presence of methanol. The reactions occurred in a short time (15-20min) and provide yields of 50-95%.

PYRAZOLE DERIVATIVE

A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

1,5-DIHETEROCYCLE-1H-TRIAZOLE DERIVATIVE

The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

PYRAZOLE DERIVATIVES

A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.

Kinetic resolution of vic-amino alcohols catalyzed by a chiral Cu(II) complex

Kinetic resolution of N-benzoylated vic-amino alcohols was achieved by benzoylation in the presence of copper triflate and (R,R)-Ph-BOX as catalysts. The observed enantioselectivity was moderate to high. The method was applied to a kinetic resolution of r

A convenient reduction of substituted amino-acid esters

Esters having N-alkyl-N-acyl (orthioacyl) functionality at the α-position are smoothly reduced with NaBH4-MeOH at 0-5°C in very good yields.

Heterocyclic compounds

Heterocyclic compounds of the general formula: STR1 wherein Z represents methylene group or sulfur atom, R represents a general formula: G represents a carbocyclic or heterocyclic ring.

Enantioselective epoxidation of unfunctionalized simple olefins by non-racemic molybdenum(VI)(oxo-diperoxo) complexes

Molybdenum(VI)(oxo-diperoxo) complexes bearing bidentate ligands with hydroxy and carbonyl functions show asymmetric induction in the stoichiometric epoxidation of simple prochiral olefins.The influence of the ligand and alkene structure on the enantiomeric excess of the oxiranes has been investigated.The addition of chiral diols to the molybdenum(VI)(oxo-diperoxo) reagents gives high enantiomeric excesses probably because of an efficient kinetic resolution of the oxiranes formed.