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.

The present disclosure provides methods for purified Plecanatide by a two-step purification method, novel intermediates that may be used in the preparation of Plecanatide, and purified Plecanatide compositions.

The present disclosure relates generally to the field of polypeptide synthesis, and more particularly, to a linear solution phase synthesis of the Wnt hexapeptide Foxy-5 and protected derivatives and peptide fragments thereof.

A salt of a phenylpropionamide derivative and a preparation method therefor is described. Specifically, the salt of the compound of formula (I) has good stability, and can be better used in clinical treatment. The process for preparing the salt of the compound of formula (I) of the present invention is simple and easy to operate. ##STR00001##

The present invention relates to an improved process for the preparation of Cetrorelix acetate (1). More particularly, the present invention relates to the purification of Cetrorelix acetate (1) by simple method. ##STR00001##

A structure of the compound containing a diphenylmethane structure of the present invention is represented by General Formula (1). The compound containing a diphenylmethane structure of the present invention contains a hydroxyl group, an amino group, a substituted amino group, and an active group, and can be used as an amino acid or peptide C-terminal protection reagent. A peptide synthesis reaction using this protection carrier has a fast reaction speed and a high reagent utilization rate in a suitable solvent system; post-treatment is carried out by means of simple liquid-liquid extraction separation, i.e. effective purification can be carried out, and finally, a product with a high purity can be obtained; and during a synthesis process, the change in solubility is small and an operation process has a strong universality, and therefore, the present method can be developed into a universal production method.

The object of the present invention is to provide a method for manufacturing an amino acid polymer more simply and efficiently compared to conventional methods for manufacturing amino acid polymers. The present invention provides a method for manufacturing an amino acid polymer with thioacid amino acids. Specifically, the manufacturing method of the present invention comprises (A) a step of preparing first and second thioacid amino acids, (B) a step of subjecting said first and second thioacid amino acids to an oxidation reaction to obtain an amino acid polymer linked by peptide bonds. The manufacturing method of the present invention is characterized in that it partially uses thioacid amino acids that do not possess a protecting group.

The object of the present invention is to provide a method for manufacturing an amino acid polymer more simply and efficiently compared to conventional methods for manufacturing amino acid polymers. The present invention provides a method for manufacturing an amino acid polymer with thioacid amino acids. Specifically, the manufacturing method of the present invention comprises (A) a step of preparing first and second thioacid amino acids, (B) a step of subjecting said first and second thioacid amino acids to an oxidation reaction to obtain an amino acid polymer linked by peptide bonds. The manufacturing method of the present invention is characterized in that it partially uses thioacid amino acids that do not possess a protecting group.

The present disclosure relates to peptide compounds and conjugate compounds, processes, methods and uses thereof for treating cancer. For example, the compounds can comprise compounds of formula TABLE-US-00001 X.sub.1X.sub.2X.sub.3X.sub.4X.sub.5GVX.sub.6AKAGVX.sub.7NX.sub.8FKSESY (SEQ ID NO: 1) (I) (X.sub.9).sub.nGVX.sub.10AKAGVX.sub.11NX.sub.12FKSESY (SEQ ID NO: 2) (II) YKX.sub.13LRRX.sub.14APRWDX.sub.15PLRDPALRX.sub.16X.sub.17L (SEQ ID NO: 3) (III) YKX.sub.18LRR(X.sub.19).sub.nPLRDPALRX.sub.20X.sub.21L (SEQ ID NO: 4) (IV) IKLSGGVQAKAGVINMDKSESM (SEQ ID NO: 5) (V) IKLSGGVQAKAGVINMFKSESY (SEQ ID NO: 6) (VI) IKLSGGVQAKAGVINMFKSESYK (SEQ ID NO: 7) (VII) GVQAKAGVINMFKSESY (SEQ ID NO: 8) (VIII) GVRAKAGVRNMFKSESY (SEQ ID NO: 9) (IX) GVRAKAGVRN(Nle)FKSESY (SEQ ID NO: 10) (X) YKSLRRKAPRWDAPLRDPALRQLL (SEQ ID NO: 11) (XI) YKSLRRKAPRWDAYLRDPALRQLL (SEQ ID NO: 12) (XII) YKSLRRKAPRWDAYLRDPALRPLL (SEQ ID NO: 13) (XIII) wherein X.sub.1 to X.sub.21 and n can have various different values and wherein at least one protecting group and/or at least one labelling agent is optionally connected to said peptide compound at an N- and/or C-terminal end.

Methods of producing a peptide containing an N-substituted amino acid or N-substituted amino acid analog of the present invention include the steps of: preparing an Fmoc-protected amino acid, an Fmoc-protected amino acid analog, or an Fmoc-protected peptide; deprotecting a protecting group which have an Fmoc skeleton of the Fmoc-protected amino acid and such by using a base; and forming an amide bond by adding a new Fmoc-protected amino acid and such; and when the peptide is produced by a solid-phase method, the obtained peptide is cleaved off from the solid phase under conditions of weaker acidity than TFA. Furthermore, at least one side chain of the obtained peptide has a protecting group that is not deprotected under basic conditions and is deprotected under conditions of weaker acidity than TFA.