METHODS FOR PREPARING MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES
申请人:Bristol-Myers Squibb Company
公开号:EP2627662A1
公开(公告)日:2013-08-21
[EN] METHODS FOR PREPARING MACROCYCLES AND MACROCYCLE STABILIZED PEPTIDES<br/>[FR] PROCÉDÉS DE PRÉPARATION DE MACROCYCLES ET PEPTIDES STABILISÉS PAR DES MACROCYCLES
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2012051405A1
公开(公告)日:2012-04-19
The invention provides methods of preparing macrocycles including macrocycle stabilized peptides (MSPs). Macrocycles and MSPs are prepared according to nucleophilic capture of an iminoquinomethide type intermediate generated from a suitably substituted 2-amino-thiazol-5-yl carbinol. The preferred nucleophile may be selected from an electron rich aromatic moiety in the case of macrocycles and, in the case of MSPs, at least one amino acid comprises an electron rich aromatic moiety. In addition, the concept can be extended to other related 5-membered heterocyclic systems in place of the thiazole, such as imidazole or oxazole. The conditions for the generation of the corresponding iminoquinomethide type intermediates may be similar or different than the conditions used for the 2-amino-thiazol-5-yl carbinol.