摘要:
A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
摘要:
An optically active (2S,5R)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxylic acid compound defined by the following formula (F): wherein R1 represents CO2R, CO2M, or CONH2, wherein R represents an allyl group or a benzyl group, and M represents a hydrogen atom, an inorganic cation, or an organic cation; and R2 represents a benzyl group or an allyl group.
摘要:
A process for producing a compound represented by a Formula (III), including reacting a compound of the following formula with a compound selected from the group consisting of 1-hydroxypyrrolidine-2,5-dione, 2-hydroxy-3a,4,7,7a-tetrahydro-1H-isoindol-1,3(2H)-dione, 2-hydroxyhexahydro-1H-isoindol-1,3(2H)-dione and 4-hydroxy-4-azatricyclo[5.2.1.02,6]dec-8-ene-3,5-dione, carrying out a carbonylation to obtain a compound of the following formula removing the NH protecting group P and treating the resultant compound with a base to produce a compound represented by the following formula wherein OBn is benzyloxy and R2 is hydrogen, ClCO— or Cl3COCO—.
摘要:
A process for producing a diazabicyclooctane derivative represented by Formula (IV) and intermediates thereof by carrying out the following steps: wherein P is an NH protecting group capable of being removed with acid; R1 is 2,5-dioxopyrrolidin-1-yl, 1,3-dioxo-3a,4,7,7a-tetrahydro-1H-isoindol-2(3H)-yl, 1,3-dioxohexahydro-1H-isoindol-2(3H)-yl, or 3,5-dioxo-4-azatricyclo[5.2.1.02.6]dec-8-en-4-yl; R2 is hydrogen, ClCO— or Cl3COCO—; R3 is C1-6 alkyl or heterocyclyl, or forms a 3- to 7-membered heterocyclic ring together with the —O—NH— to which it is attached; and OBn is benzyloxy.
摘要:
A compound of the following compound (B): wherein tBu represents a tert-butyl group. A compound of the following compound (C): wherein tBu represents a tert-butyl group, and TFA represents a trifluoroacetyl group.
摘要:
A process for preparing a diazabicyclooctane compound represented by the following formula (I): wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c): wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
摘要:
A process for producing a compound of the following Formula (VII-CR): The process involving providing a compound represented by the following Formula (VI): in a case where the R3ONHC(═O) side chain in the compound of the Formula (VI) has a protecting group, removing the protecting group from the compound of the Formula (VI) with an acid, and adding an ester-based poor solvent to the resultant reaction solution to precipitate the compound of Formula (VII-CR), wherein in the compounds of the Formulas (VII-CR) and (VI), R3 is a C1-6 alkyl or a heterocycle.
摘要:
A process for preparing a diazabicyclooctane compound represented by the following formula (I):
wherein A represents RcO—; B represents NH or NC1-6 alkyl; C represents a benzyl group; Rc represents a C1-6 alkyl group; A is substituted with one substituent Fn1, wherein Fn1 represents an azetidine group; the process including: (a) silylating the compound represented by the following formula (IV-c):
wherein in the formula (IV-c), OBn represents benzyloxy, and (b) carrying out an intramolecular urea formation reaction.
摘要:
A crystalline form I of a compound represented by Formula (VII-1): having characteristic peaks appearing at lattice spacing (d) of 7.34, 5.66, 5.53, 5.30, 5.02, 4.66, 4.37, 4.28, 4.06, 3.68, 3.62, 3.47, 3.36, 3.30, 3.16, 3.11, 3.03, 2.99 and 2.50 Å in the powder X-ray diffraction pattern.