Lonza Inc.

Lonza Ag

Polypeptide Laboratories Holding (ppl) Ab

Matthieu Giraud

Oleg Werbitzky

Fernando Albericio

Stéphane Varray

Carsten Meininghaus

Fernando Albericio Palomera

Judit Tulla-Puche

Michèle Cristau

Miriam Gongora Benitez

Deyong Tan

Albert Isidro Liobet

Mercedes Alvarez Domingo

Joanna Dai

Albert Isidro Llobet

The invention discloses a method for the preparation of N-omega-(1,2-dimethylindole-3-sulfonyl)-L-arginine and its derivatives using L-ornithine.

Method for the preparation of H-Arg(MIS)-OH

A new method of synthesizing GLP-1 peptide is devised.

Synthesis of glucagon-like peptide

The invention relates to a method for homogeneous solution phase peptide synthesis (HSPPS) of a N-terminal peptide fragment PEP-N and a C-terminal peptide fragment C-PEP, with C-PEP carrying a specific diketopiperazine (DKP) comprising C-terminal protecting group, which contains a handle group HG, with HG being connected to the C-terminus of the peptide fragment; thereby this specific DKP comprising C-terminal protecting group can be selectively cleaved from the peptide as a conventionally used C-terminal protecting group. By the use of this DKP and HG comprising C-terminal protecting group, certain process steps in convergent peptide synthesis based on a combination of HSPPS and solid phase peptide synthesis (SPPS) can be avoided. The invention relates further to a method for the preparation of such specifically protected fragment C-PEP by SPPS by using a linker comprising a specific dipeptide and HG for connecting the growing peptide chain to the resin, which linker forms said DKP group, when the peptide fragment C-PEP is cleaved from the supporting resin; and further to the intermediates of the preparation method.

Diketopiperazine forming dipeptidyl linker

The invention relates to indolesulfonyl halogenides which are useful for the protection of organic compounds comprising at least one guanidino moiety and/or at least one amino group. The invention further relates to a process for their preparation and their use as protecting reagents. The invention also relates to the process for the protecting reaction and to the protected compounds thereof.

Indolesulfonyl protecting groups for protection of guanidino and amino groups

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Sion, Switzerland

Matthieu Giraud