KR830004214A - New phosphoryl muramil peptide and its preparation - Google Patents

Abstract

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Description

New phosphoryl muramil peptide and its preparation

Since this is an open matter, no full text was included.

Claims (1)

Reacting the compound of formula (V) or a metal compound thereof with the compound of formula (VI) and removing the protective group present, or condensing the following compound of formula (V) or its derivative with compound of formula (V) or derivative And remove the existing protecting group, or condensate the compound of formula (VII) or its derivative with the compound of formula (VII), and remove the protecting group present or replace the compound of formula (XI) with compound of formula (XII) Condensation and the cleavage of the optionally present protecting group or esterification of the next compound of formula (XIa) with the compound of formula (XIIa) and the cleaving of the group of Cleave to the acid and remove any protective groups that are present or form the following compound (X IV) Condensation with the compound and the optional protecting group is removed or the following structural formula (X VII) compound is esterified with the next structural group (XIX) compound and the optional protecting group is removed or the following structural formula (XX) compound is (XXI) reacts with the compound that produces the compound and removes the existing protecting group, or reacts the following structural formula (XXIII) with the next structural formula (XXV) and removes the existing protective group, or one or more functional groups Muramyl peptides of the following formula (I) and salts thereof, characterized by the removal of these protecting groups from the compounds of formula (I) protected by the protecting group and the conversion of the resultant How to prepare. In the above formula X represents carbonyl or carbonyloxy, P ₁ represents optionally substituted alkyl or aryl, R ₂ , R ₄ and R ₆ represent hydrogen or lower alkyl, R ₃ represents hydrogen or lower alkyl, R ₅ is hydrogen, lower alkyl, free or modified hydroxy-lower alkyl, free or modified mercapto-lower alkyl, optionally substituted amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, optionally substituted aryl or Aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-loweralkyl, or R ₄ and R ₅ together represent alkylene having 3 or 4 carbon atoms, R ₇ represents hydrogen or optionally esterified or amidated carboxyl and one of A ₁ and A ₂ represents a radical of formula (II) In the formula (II) T represents -NH or -0, Y represents an optionally substituted alkylene group which may be broken into one or two oxycarbonyl and / or aminocarbonyl groups, W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical each having at least 6 carbon atoms, Z represents a reactive esterified hydroxyprotecting group, The other of A ₁ and A ₂ represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino optionally substituted in lower alkyl radicals, R ₉ , R ₁₀ and R ₁₁ represent a protective group which can be easily removed, except that structural formulas (VII), (VII), (XI) and (XIa) represent hydrogen or a readily removable protective group, One of A ₁ ^o and A ₂ ^o represents a cyclized hydroxy group and the other represents etherified hydroxy, amino, lower alkyl amino, or amino carbonyl-lower alkyl amino provided that A ₁ in formula (XIa) ^{one of o} and A ₂ ^o represents a hydroxy group instead of an activated hydroxy group, R ₁₂ represents an alkylidene or cycloalkylidene group, one of A ₁ ′ and A ₂ ′ is a radical of the formula (XV), -TY ₁ -M ₁ (XV) The remainder is etherified hydroxy or amino, lower alkyl amino or aminocarbonyl-lower alkyl amino, One of M ₁ and M ₂ represents a free amino group or an active derivative thereof, Y ₁ and Y ₂ each represent an optionally substituted lower alkylene, One of A ₁ "and A ₂ " is a radical of the following formula (XVIII) Any hydroxy group present at Y ₁ is protected by a readily removable group -TY ₁ -M ₃ (XVIII) Others represent etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkyl amino, One of M ₃ and M ₄ represents a free hydroxy group and the other represents a free carboxyl group, with one radical optionally present in a reactive form, wherein A ₁ "'and A ₂ in structural formulas (XX) and (XXI) One of "'represents -TY-OH and the other radical represents free or esterified hydroxy, amino or lower alkyl amino, or A ₁ ""and A ₂ in structural formula (XXIII) optionally substituted in lower alkyl radicals; One of "" represents the following structural formula (XXIV) The rest represent free or etherified hydroxy, amino, lower alkyl amino or aminocarbonyl-lower alkyl amino Y and T are as described above, M ₅ represents an electron pair or oxo, if M ₅ represents an electron pair, it is oxidized by a weak oxidizer, M ₆ represents hydrogen or an easily removable protective group, M ₇ represents a hydroxy group optionally present in the form of a reaction. ※ Note: The disclosure is based on the initial application.