| 摘要 |
<p>1,201,053. Corticotropines. RICHTER GEDEON VEGYESZETI GYAR RT. 8 Sept., 1967 [10 Sept., 1966; 28 March, 1967], No. 41232/67. Heading C2C. A process for the synthetic preparation of the human corticotropine (I) H-Ser (1) -Tyr (2) - Ser (3) - Met (4) - Glu (5) - His (6) - Phe (7) - Arg (8) - Try (9) - Gly (10) - Lys (11) - Pro (12) - Val (13) - Gly (14) - Lys (15) - Lys (16) - Arg (17) - Arg (18) - Pro (19) - Val (20) - Lys (21) - Val (22) - Tyr (23) - Pro (24) - Asp (25) - Ala (26) - Gly (27) - Glu (28) - Asp (29) - Gly (30) - (NH 2 ) - Ser (31) - Ala (32) - Glu (33) - Ala (34) - Phe (35) - Pro (36) - Leu (37) - Glu (38) - Phe (39) - OH and the analogous pig-, bovine- and sheep-corticotropines wherein the sequence 25-33 of the amino acids in the above formulais replaced by- Asp (25) - Gly (26) - Ala (27) - Glu (28) - ASP (29) - Glu (30) (NH 2 ) - Leu (31) - Ala (32) - Glu (33) -, -Asp (25) - Gly (26) - Glu (27) - Ala (28) - Glu (29) - Asp (30) - Ser (31) - Ala (32) - Glu(NH 2 ) (33) - or - Ala (25) - Gly (26) - Glu (27) - Asp (28) - Asp (29) - Glu (20) - Ala (31) - Ser (32) -Glu(NH 2 ) (33) - respectively and also of the fragments H - Ser - Tyr - Ser - Met - Glu - His - Phe - Arg - Try - Gly - Lys - Pro - Val - Gly-Q-T which contain at least the first 15 aminoacids of the above corticotropines [T is OH or NH 2 and Q is an appropriately protected amino acid sequence (15-39) of the natural corticotropines or any fragment of the said sequence (15-39)] comprises coupling an appropriately protected polypeptide which is claimed per se comprising the sequence (1-14) of (I) with a suitably protected peptide of the formula H-Q-T<SP>1</SP> (where T<SP>1</SP> is NH 2 , alkoxy or aryloxy) using methods known per se in peptide chemistry. The thus-obtained corticotropine or corticotropine fragment is then treated to remove the protecting groups by methods known per se. The intermediate peptides described are those comprising the following sequences of amino acids of compound (I): (20-32), (15-32), (31-36), (30-36), (30-39), (29-39), (28-39), (26-27), (25-27), (25-39), (17-19), (15-16), (15-19), (23-24), (22-24), (21-24), (20-24), (15-24), (15-39), (9-14), (8-14), (5-7), (5-14), (28-32), (20-27), (20-39), (1-15), (1-16), (15-17), (1-17), (15-18), (1-18), (15-19), (1-19), (1-32), (15-20), (1-20), (15-21), (1-21), (26-28), (25-28), (20-28), (15-28), (1-28), (31-32), (30-32) and (29-32) and the following sequences of amino acids of the corresponding pig corticotropine: (26-28), (25-28), (20-28) and (15-28). The compounds Z-Tyr(Bu<SP>t</SP>)OSu, Z-Lys(BOC)OSu, Z-Asp(OBu<SP>t</SP>)ONSu and Z-Glu(NH 2 )-OPCP are also formed.</p> |
