As a water-soluble azole Antifungal Spectrum, a process for their PreparationA Broker and a Pharmaceutical composition comprising the same and use in the preparation of a medicament

摘要

1 Soluble azoles (I) in formula,A form of positive oxidation, a pharmaceutically acceptable addictive salt, or a three-dimensional structure that is chemically identical, in which l represents a radical choice from formula to (f),in which Alk independently represents a C1-6 alkanediyl optionally substituted with hydroxy or C1-4 alkyloxy, n is 1,2 or 3; Y is O, S or NR2; R1 represents H, aryl, Het1 or a C1-6alkyl optionally substituted with 1, 2 or 3 substituents, each of which is independently selected from halo, hydroxy, mercapto, C1-4alkyloxy, C1-4alkylthio, aryloxy, arylthio, C1-4 arylalkyloxy, C1-4 arylalkylthio, cyano, amino, mono- or di (C1-4alkyl) amino, mono- or diarylamino, mono-odi (ari lalkyl) C1-4, amino, C1-4 alkyloxycarbonylamino, benzyloxycarbonylamino , aminocarbonyl, carboxyl, C1-4 alkyloxycarbonyl, guanidyl, aryl, or Het2; each R2 independently represents H,or C1-6alkyl, or if R1 and R2 are attached to the nitrogen atom, they can be taken together to form a heterocyclic radical selected from morpholinyl, pyrrolidinyl, piperidinyl, homopeperidinyl or piperazinyl; said heterocyclic radical may be optionally substituted with C1-4alkyl, aryl, Het2, arylalkyl C1-4, Het2 C1-4alkyl, hydroxyalkyl C1-4, amino, mono- or dialkyl C1-4 amino, aminoalkyl C1-4, mono- or dialkyl C1-4aminoalkyl, carboxyl, aminocarbonyl, C1-4alkyloxycarbonyl, C1-4alkyloxycarbonylamino, or mono- or dialkyl C1-4 aminocarbonyl may be taken together to form an azido radical; each R3 independently represents H,hydroxy or C1-4 alkyloxy; aryl represents phenyl, naphthalenyl, 1,2,3,4-tetrahydronaphthalenyl, indenyl, or indanyl; each or one of said aryl groups may be optionally substituted with one or more substituents selected from halo, C1-4alkyl, hydroxy, C1-4alkyloxy, nitro, amino, trifluoromethyl, hydroxyalkyl, C1-4alkyl, C1-4alkyl, aminoalkyl C 1-4, mono- or dialkyl C1-4 aminoalkyl C1-4; Het1 represents a monocyclic or bicyclic substituted heterocyclic radical; the radical