| PATENT ASSIGNEE'S COUNTRY | USA |
| UPDATE | 09.99 |
| PATENT ASSIGNEE | This data is not available for free |
| PATENT CLAIMS |
Claim 12: Method of synthesizing & cyclizing cyclosporin or analog on solid support - Covalently bonding a side chain of an aminoacid corres ponding to position-3 or position-7 of the cyclosporin or analog to be synthesized to solid support via a mild-acid labile or photo-labile linker to yield a support-bound residue having N-terminus & C-terminus - Protecting the C-terminus of support-bound residue - Sequentially coupling C-termini of adjacent aminoacids to be incorporated into the cyclosporin or analog to the N-ter minus of the support-bound residue to yield a support- bound linear peptide having N-terminus - Repeating above step to yield linear analog & wherein when aminoacids corresponding to position-11 through position-8 of the cyclosporin or analog are coupled the coupling is accomplished using a solvent comprising N-Me pyrrolidinone in excess at T = 40C to boiling point of solvent at atm pressure - Deprotecting the C-terminus of support-bound residue & cyclizing the linear analog by treating it with a reaction soln comprising benzotriazolyl-N-oxy-tris(dimethylamino)phos phonium hexafluorophosphate to yield a support-bound cyclosporin or analog |
| PATENT PHOTOCOPY | Available on request |
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