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:ES-2333781-T3 优先权日:2001-09-07 标 题 :SYNTHESIS PROCEDURES OF INSULIN-OLIGOMERO POLYPEPTIDE CONJUGATES AND PROINSULIN-OLIGOMERO POLYPEPTIDE CONJUGATES, AND SYNTHESIS PROCEDURES OF THE SAME.
参考文献:10.1055/s-2005-918931 摘要:Knochel P, Gommermann N, Gehrig A. Enantioselective Synthesis of Chiral α-Aminoalkyl-1,2,3-triazoles Using a Three-Component Reaction. Synlett. 2005;(18):2796–8. doi: 10.1055/s-2005-918931.