Pyrrolidin-2-one derivative

Pyrrolidin-2-one derivatives, (III), prepared by Chan (3) were effective as factor Xa inhibitors and useful in treating diseases associated with coronary thrombosis. 

The reaction of MBFI adduct with alkane-amines also provided an effective protocol to synthesize pyrrolidin-2-one derivatives via nucleophilic reaction and subsequent cyclization processes. Ayed et al. first reported the direct condensation of MBH adduct with primary amines in methanol to afford 3-hydroxyl pyrrolidin-2-ones 410 in good to excellent yields (Scheme 4.130). The reaction of (5)-phenylethylamine with MBH adduct 411 was reported to generate an equimolar mixture of the 4,5-ci5-disubstituted pyrrolidin-2-ones 412 and 413 (Scheme 4.131). Interestingly, pyrrolidin-2-one 413 could be further used to synthesize the glycosidase inhibitor 414. ... 

Sathiyanarayanan et al. [31] developed a simple and efficient three-component domino reaction of y-butyrolactam (2-pynolidinone), aromatic aldehyde, and substituted thiophenol catalyzed by iodine for the synthesis of l-((phenylthio)(phenyl) methyl)pyrrolidin-2-one derivatives 8. The stability of the synthesized analogs was evaluated in stimulated gastric fluid (SGF) and bovine serum albumin (BSA Scheme 10.6). 

Ramachandran G, Karthikeyan NS, Giridharan P, Sathiyanarayanan KI (2012) Efficient iodine catalyzed three components domino reaction for the synthesis of l-(phenylthioXphe-nyl)methyl)pyrrolidin-2-one derivatives possessing anticancer activities. Org Biomol Chem 10 5343-5346... 

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See also in sourсe #XX -- [ , , , , , , , , , ]

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