A peptide having a fluoroalkyl group as its side chain and a method for producing, which comprises condensing a compound represented by the formula (6-2) or (6-4), where means that an asymmetric carbon atom has an absolute configuration of S or R, Rf is a C.sub.1-30 alkyl group which is substituted with at least two fluorine atoms, and which may further be substituted with a halogen atom other than a fluorine atom (when the C.sub.1-30 alkyl group is a C.sub.2-30 alkyl group, it may have 1 to 5 etheric oxygen atoms between carbon atoms), and R.sup.2 is a protecting group for the amino group, with a fluorinated amino acid having its carboxy group protected, an amino acid having its carboxy group protected, a fluorinated peptide having its C-terminal protected, or a peptide having its C-terminal protected.

The present inventors found that peptide compounds/amide compounds in which the protecting groups of interest are removed and/or which are removed from resins for solid-phase synthesis can be produced without main chain damage by contacting starting peptide compounds/amide compounds with silylating agents.

The present inventors found that peptide compounds/amide compounds in which the protecting groups of interest are removed and/or which are removed from resins for solid-phase synthesis can be produced without main chain damage by contacting starting peptide compounds/amide compounds with silylating agents.

The present invention comprises conjugates comprising a monoclonal antibody conjugated to a cyclic PYY peptide. The invention also relates to pharmaceutical compositions and methods for use thereof. The novel conjugates are useful for preventing, treating or ameliorating diseases and disorders disclosed herein.

The present invention relates to methods and compounds for the solid phase synthesis of peptides carrying a substituent at an amino group of an amino acid side chain.

The present inventors found that peptide compounds/amide compounds in which the protecting groups of interest are removed and/or which are removed from resins for solid-phase synthesis can be produced without main chain damage by contacting starting peptide compounds/amide compounds with silylating agents.

The present inventors found that peptide compounds/amide compounds in which the protecting groups of interest are removed and/or which are removed from resins for solid-phase synthesis can be produced without main chain damage by contacting starting peptide compounds/amide compounds with silylating agents.

The present invention provides a method for preparing S-Bz-MAG3 as a precursor of contrast media. Thioglycolic acid and benzoyl chloride are taken for the thiol protection reaction. Next, N,N′-dicyclohexylcarbodiimide and N-hydroxysuccinimide are converted to corresponding ester compounds. The corresponding ester compounds then react with triglycine by amide bonding reaction. The product of the reaction is recrystallized using acetone, filtered, and finally flushed using flushing agent to give the final product. This is a bifunctional chelator and can be bridged with 99mTc and 186/188Re effectively and applied to nuclear medicine imaging and tumor radiotherapy. By taking advantage of fewer synthesis steps and ease of operations, complicated separation and purification reactions can be reduced and thus achieving highly productivity of S-Bz-MAG3.

In a preferred embodiment, there is provided a protecting group for protecting the thiol side chain of a cysteine residue, the protecting group comprising a Diels-Alder cycloadduct of a furan and a maleimide, and optionally, a linker interposed between the thiol side chain and the Diels-Alder cycloadduct.

Described herein is a process for the total synthesis of macrolactones and macrolactams of formula I ##STR00001##
including E- and Z-configuration thereof, in particular, nannocystins.