| US 7,615,609 B2 | ||
| Preparation of somatostatin peptides | ||
| Heribert Hellstern, Heitersheim (Germany); Werner Pachinger, Basel (Switzerland); Walter Prikoszovich, Schoenenbuch (Switzerland); and Bernhard Wietfeld, Efringen-Kirchen (Germany) | ||
| Assigned to Novartis AG, Basel (Switzerland) | ||
| Appl. No. 10/567,299 PCT Filed Aug. 06, 2004, PCT No. PCT/EP2004/008850 § 371(c)(1), (2), (4) Date Feb. 06, 2006, PCT Pub. No. WO2005/014624, PCT Pub. Date Feb. 17, 2005. |
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| Claims priority of application No. 0318682.2 (GB), filed on Aug. 08, 2003. | ||
| Prior Publication US 2006/0258838 A1, Nov. 16, 2006 | ||
| Int. Cl. C07K 7/64 (2006.01) | ||
| U.S. Cl. 530—317 [530/333] | 3 Claims |
1. A process for producing a compound of formula I
 R1 is —C2-6alkylene-NR3R4, —C2-6alkylene-guanidine or —C2-6alkylene-COOH wherein each of R3 and R4 independently is H, C1-4alkyl, ω-hydroxy-C2-4alkylene oracyl or R3 and R4 form together with the nitrogen atom to which they are attached a heterocyclic group which may comprise a further heteroatom,
and
R2 is Z1-CH2—R5, —CH2—CO—O—CH2—R5,
 wherein Z1 is O or S and R5 is optionally substituted phenyl,
or a salt thereof,
comprising cyclizing a linear somatostatin analogue of formula II
 with a cyclizing agent selected from O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium-hexaflurophosphate and 1-hydroxybenzotriazole,
wherein R1 and R2 are as defined above,
each of R11 and R12, independently, is an amino protecting group
whereby when R1 comprises a terminal NH2, this terminal NH2 is also protected by an amino protecting group,
and where required removing the protecting group(s),
and recovering a compound of formula I thus obtained in free form or in salt form.
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