专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-4212795-A 优先权日:1978-11-13 标题:Cyclization of peptides 发明人:HUGHES JOHN L; LIU ROBERT C; SEYLER JAY K 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing two cysteine moieties, each of which is protected by an n-alkylthio group, or when one of such moieties is in an amino terminal position, this one moiety may be protected by a cysteine group while the other is protected by an n-alkylthio group, and placing such intermediate peptide in a solution substantially free of oxygen and preferably at a pH of from 5 to 10 until rearrangement has taken place, to yield a cyclic disulfide peptide. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:US-4033940-A 优先权日:1975-11-12 标 题:Cyclization of peptides 发明人:HUGHES JOHN L; SEYLER JAY K; LIU ROBERT C 权利人:ARMOUR PHARMA 摘要:The synthesis of a disulfide cyclic peptide by preparing an intermediate peptide containing an amino terminal cystine residue and a cysteine residue located in a position within the amino acid sequence, to give a desired peptide, and placing such intermediate peptide in a solution substantially free of oxygen at a pH of from about 5 to 10 until rearrangement takes place to yield a cyclic disulfide peptide and to displace a molecule of cysteine from the amino terminal cysteine residue. The disclosure also embraces said intermediate peptides as new compounds and the processes by which they are prepared.
专利号:US-4089821-A 优先权日:1976-03-31 标 题:Synthesis of peptide amides 发明人:ENKOJI TAKASHI; SKIBBE MARTIN O 权利人:ARMOUR PHARMA 摘要:Peptide amides having biological activity and resin peptide amides useful in the preparation of peptides having biological activity, particularly such peptides containing the structure in which R is divinylbenzene crosslinked polystyrene and Bz is benzyl, p-methoxybenzyl, p-chlorobenzyl, p-nitrobenzyl, or benzhydryl, and in which phe and glu are residues of the amino acids phenylalanine and glutamic acid; and processes for preparing such peptide amides.
专利号:US-3592836-A 优先权日:1966-12-23 标 题:Aryloxycarbonyl fluorides and amino acids and their production 发明人:UGI IVAR; KLAUKE ERICH; SCHNABEL EUGEN; HOFFMANN PETER 权利人:BAYER AG 摘要:ARYLOXYCARBONYL FLUORIDES SUCH AS FURFURYLOXYCARBONYL-, P-METHOXYBENZYLOXYCARBONYL- AND TRIMETHOXYBENZYLOXYCARBONYL-FLUORIDES ARE PROVIDED WHICH ARE USEFUL AS INTERMEDIATES FOR AMINO ACID DERIVATIVES AND ARE OBTAINED FROM CARBONYL-FLUORIDE CHLORIDE BY REACTION WITH THE APPROPRIATE ALCOHOL. THE AMINO ACID DERIVATIVES OF SUCH CARBONYL-FLUORIDES ARE BUILT UP THROUGH ACYLATION OF AMINO ACIDS THEREWITH. THESE AMINO ACID DERIVATIVES ARE USEFUL AS INTERMEDIATES FOR THE SYNTHESIS OF POLYPEPTIDES. THE REACTION OF CARBONYLCHLORIDE-FLUORIDE IS ADVANTAGEOUSLY CARRIED OUT AT TEMPERATURES OF 0 TO 70*C. IN AN INERT SOLVENT AND IN THE PRESENCE OF AN ACID-BINDING AGENT. THE AMINO ACID DERIVATIVES ARE FORMED AT TEMPERATURES BETWEEN +20 AND -20*C. ALSO IN THE PRESENCE OF AN ACID-BINDING AGENT. IMINO ACIDS CAN BE USED IN PLACE OF AMINO ACIDS. THE AMINO- OR IMINO-ACID DERIVATIVES OR ESTERS ARE ADVANTAGEOUSLY PREPARED AT CONSTANT. CONTROLLED PH VALUES, PREFERABLY BY THE USE OF AUTOMATIC PH CONTROL EQUIPMENT.
专利号:GB-1586974-A 优先权日:1977-07-04 标 题:Synthesis of peptide amides