METHODS OF SYNTHESIZING LIPSTATIN DERIVATIVES

Provided according to embodiments of the invention are methods of forming a lipstatin derivative, (S)-1-((2S,3S)-3-ethyl-4-oxooxetan-2-yl) tridecan-2-yl formyl-L-alaninate. Such methods include one or more reaction steps that include the Mitsunobu coupling of N-formyl L-alanine in the presence of di...

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Bibliographische Detailangaben
Hauptverfasser:	LEE, Gary, Richard, BOKKA, Apparao, AKURATHI, Gopalakrishna, KAMAL, Zeeshan
Format:	Patent
Sprache:	eng ; fre ; ger
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	Provided according to embodiments of the invention are methods of forming a lipstatin derivative, (S)-1-((2S,3S)-3-ethyl-4-oxooxetan-2-yl) tridecan-2-yl formyl-L-alaninate. Such methods include one or more reaction steps that include the Mitsunobu coupling of N-formyl L-alanine in the presence of di-t-butyl azodicarboxylate (DBAD) and triphenylphosphine. Compounds formed by a method of the invention, compositions that include a compound formed by a method of the invention, and methods of inhibiting lipase activity and/or treating pancreatitis using a compound formed by a method of the invention are also provided.