PROCESS FOR THE PREPARATION OF AZACYCLOALKYLALKANOYL PSEUDOTETRAPEPTIDES

1. A process for preparing a pseudotetrapeptide compound of formula or a salt or prodrug thereof wherein is optionally amino protected 4-8 membered azaheterocyclyl; is a single or double bond; q is 1-5; B is C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkylC1-C20alkyl, C1-C20alkylC3-C10cycloalkyl, C1-...

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Bibliographische Detailangaben
Hauptverfasser:	MENCEL, JAMES, J, LAVIGNE, MICHEL, DAUBIE, CHRISTOPHE, LEON, PATRICK, VANASSE, BENOIT, J, LIU, ROBERT, C, STAMMLER, ROBERT, D'NETTO, GEOFFREY, A
Format:	Patent
Sprache:	eng ; rus
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEPTIDES PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:	1. A process for preparing a pseudotetrapeptide compound of formula or a salt or prodrug thereof wherein is optionally amino protected 4-8 membered azaheterocyclyl; is a single or double bond; q is 1-5; B is C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkylC1-C20alkyl, C1-C20alkylC3-C10cycloalkyl, C1-C20alkylC3-C10cycloalkylC1-C20alkyl, C6-C10aryl, C6-C10arC1-C20alkyl, C1-C20alkylC6-C10aryl or C1-C20alkylC6-C10arC1-C20alkyl; Q2 is H or a carboxy protecting group; J is -H, C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkylC1-C20alkyl, C1-C20alkylC3-C10cycloalkyl, C1-C20alkylC3-C10cycloalkylC1-C20alkyl, C6-C10aryl, substituted C6-C10aryl, C6-C10arC1-C20alkyl or substituted C6-C10arC1-C20alkyl; L is OR , or NR R , where R and R are independently -H, C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkyl C1-C20alkyl,C1-C20alkyl C3-C10cycloalkyl, C1-C20alkyl C3-C10cycloalkyl C1-C20alkyl, C6-C10aryl, C6-C10ar C1-C20alkyl,C1-C20alkyl C6-C10aryl, or C1-C20alkyl C6-C10ar C1-C20alkyl, and p is 1 or 2, comprising (a) coupling an azaheterocyclyl pseudodipeptide of formula or a salt thereof wherein K is OH or an acyl activating group, with a carboxylic acid substituted dipeptide of formula or a salt thereof; (b) optionally removing the amino protecting group or carboxylic acid protecting group and (c) optionally converting the pseudotetrapeptide to the salt or prodrug. 2. The process of Claim 1 wherein is a group of formula wherein m is 1 to 5, preferably 3; n is 2-6, preferably 3 or 4; and P1 is an amino protecting group, wherein Q2 is a carboxy protecting group; wherein B is C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkylC1-C20alkyl, C1-C20alkyl C3-C10cycloalkyl, or C1-C20alkyl C3-C10cycloalkyl C1-C20alkyl, J is -H, C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkyl C1-C20alkyl,C1-C20alkyl C3-C10cycloalkyl, or C1-C20alkyl C3-C10cycloalkyl C1-C20alkyl. 3. The process of Claim 2 wherein B is C1-C20alkyl, J is C1-C20alkyl, C3-C10cycloalkyl, or C3-C10cycloalkyl C1-C20alkyl, R and R are independently -H, C1-C20alkyl, C3-C10cycloalkyl, C3-C10cycloalkyl C1-C20alkyl, C1-C20alkyl C3-C10cycloalkyl, C1-C20alkyl C3-C10cycloalkyl C1-C20alkyl or C6-C10ar C1-C20alkyl, m is 3, n is 3 or 4, and p is 1. P1 is benzyloxycarbonyl and Q2 is H or benzyl, L is -NR R . 4. The process of Claim 1 wherein the salt of the azaheterocyclyl pseudodipeptide is coupled with the salt of the carboxylic acid substituted dipeptide or wherein a base addition salt of the azaheterocyclyl pseudodipeptide is coupled with an