| abstract |
REFERS TO ANTIBACTERIALS OF GENERAL FORMULA (I), WHERE: R1 IS N3, OH, OR2, OSO2R3 OR NR4R5; R2 IS ACIL (C1-C8), AMONG OTHERS; R3 IS ALKYL (C1-C4), AMONG OTHERS; R4 AND R5 ARE H, CYCLLOALKYL (C3-C6), (ALKYL OR ALCOXY) (C1-C6) or -COR6, AMONG OTHERS; R6 IS CYCLOALKYL (C3-C6) OPTIONALLY SUBSTITUTED OR IS (ALCOXY, ALKYL OR ALKYLLIN) (C1-C6) LINEAR OR BRANCH, AMONG OTHERS; "A" IS (II), AMONG OTHERS, WHERE: "G", "L" AND "M" ARE H; "D" IS O or S; "E" IS O, S, or NH; R12 IS H or (RENT OR ALKYLENE) (C1-C10) LINEAR OR BRANCH, AMONG OTHERS. IT ALSO REFERS TO THE PRODUCTION PROCEDURES OF (I), WHICH INCLUDE: 1) TREATING AN = C = O, A-CO-N3 OR A-NH-CO2-X (X IS PROTECTIVE GROUP) WITH EPOXIDE (III) ; AND IF R1 IS OH, RELEASE THE OH FUNCTION BY SAPONIFICATION OR TRANSESTERIFICATION; 2) IF R1 IS OH, TREAT A-CO-N3 WITH ALCOHOL, OBTAINING A-NH-CO2-Y (AND IS PREFERABLY n-BUTYL); THEN GO ON TO STEP 1; 3) TREAT (IV) WITH ACID AND DIETHYL CARBONATE, OBTAINING A-NH-CH2-CHOH-CH2OH, THEN CYCLE IN THE PRESENCE OF A COADJUVANT AGENT; 4) TREAT (I), WHERE R1 IS OH WITH: (1�) Cl- (ALQUIL-O-FENIL-SULFONILO), (2�) NaN3, (3�) (CH3O) 3P, (4�) ACCILLATING AGENT , FOR R1 TO BE NH-CO-R6; 5) CYCLE TO GET "A"; 6) COUPLING THE REST "A" TO (I), (IF R12 IS NOT H AND R1 IS NH-CO-CH3, IT IS OILED OR RENTED WITH DISPLACEMENT OF THE DOUBLE LINK) |