Following is one of the patent documents most requested by researchers using CAS electronic products.
|
CAS indexed 28 chemical substances from this document.
CAS subject entries for this document include: Peptides, preparation; Amidation. | |
CAPLUS COPYRIGHT 2006 ACS on STN
| TITLE:
| Method for the synthesis of peptide amides |
| INVENTOR(S):
| Giraud, Matthieu; Williner, Michaela; Werbitzky, Oleg |
| PATENT ASSIGNEE(S):
| Lonza AG, Switz. |
| SOURCE:
| PCT Int. Appl., 24 pp. CODEN: PIXXD2 |
| LANGUAGE:
| English |
PATENT INFORMATION: PATENT NO. KIND DATE APPLICATION NO. DATE
--------------- ---- -------- -------------------- --------
WO 2006008050 A1 20060126 WO 2005-EP7625 20050713
W: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH,
CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD,
GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KP, KR, KZ,
LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA,
NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK,
SL, SM, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU,
ZA, ZM, ZW
RW: AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE,
IS, IT, LT, LU, LV, MC, NL, PL, PT, RO, SE, SI, SK, TR, BF, BJ,
CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG, BW, GH,
GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW, AM, AZ, BY,
KG, KZ, MD, RU, TJ, TM
ABSTRACT:
A novel method for amidation of the C-terminal carboxyl group of peptides avoids undesired epimerization of the .alpha.-carbon of the C-terminal amino acid yielding diastereoisomeric variants of the amidated peptide. The method involves reaction of an .alpha.-amino group-protected peptide with a coupling reagent in an org. solvent in the presence of a base and an ammonium salt. Thus, peptide ILRWPWWPWRRK-OH was Boc protected at the N-terminus and the .epsilon.-amino group of lysine and treated with HCTU, N-methylmorpholine and NH2/HOOBt in DMF to afford the peptide amide, following deprotection.
Updated 5/8/2007 1:29:27 PM
