57451-90-8

Upstream product

• 32315-10-9 bis(trichloromethyl) carbonate 
• 57451-91-9 1-benzenesulfonyl-imidazolidin-2-one 
• 503-38-8 trichloromethyl chloroformate 

Relevant academic research and scientific papers

The preparation of 3-substituted 1-chlorocarbonyl-imidazolidin-2-ones using bis(trichloromethyl) carbonate

A novel synthesis of 3-substituted 1-chlorocarbonyl-imidazolidin-2-ones using bis(trichloromethyl) carbonate is reported. The bis(trichloromethyl)carbonate is used to generate phosgene in situ in stoichiometric amounts. The yields and purity of the products obtained are better than those obtained by a conventional way using phosgene.

Cephalosporins and their production

Cephalosporins of the formula STR1 their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, wherein A is hydrogen; unsubstituted or substituted alkyl; aryl; or R1 --X--, wherein X is --CO-- or --SO2 --, and R1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl; Or when X is --CO--, R1 can also be alkoxy; B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety STR2 E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality. These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

Oxo-imidazolidine substituted cephalosporins and antibacterial compositions and methods of combatting bacteria employing them

Cephalosporins of the formula STR1 their pharmaceutically-acceptable, nontoxic salts, and hydrates thereof are produced, wherein A is hydrogen; unsubstituted or substituted alkyl; aryl; or R1 --X--, wherein X is --CO-- or --SO2 --, and R1 is hydrogen, unsubstituted or substituted alkyl; aryl; thienyl; furyl; amino; alkylamino; dialkylamino; pyrrolidyl; or piperidyl; Or when X is --CO--, R1 can also be alkoxy; B is phenyl, methylphenyl, chlorophenyl, hydroxyphenyl or the moiety STR2 E is hydrogen, hydroxyl or acetoxy; and C is a center of chirality. These compounds are particularly useful for their antimicrobial and, particularly, antibacterial effects.

Penicillins

Penicillins of the formula EQU1 or pharmaceutically acceptable non-toxic salts thereof, wherein C is a carbon atom constituting a center of chirality; A is a moiety of the formula EQU2 or EQU3 wherein X is EQU4 Y is EQU5 or wherein Aryl is an aryl moiety; Z is EQU6 Q1 is EQU7 or SPC1 Q2 is EQU8 SPC2 or SPC3 R is straight-chain or branched alkyl of 1 to 5 carbon atoms; R1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms, vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H2 N--, R--NH--, (R)2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S-- V--, N=C--V--, R--O--CO--V--, H2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO2 --NH--, (R)2 N--CO--V--, wherein R is as above defined, SPC4 SPC5 provided that when X is --SO2 --, R1 is not alkoxy, aralkoxy, cycloalkoxy or aryloxy, and further provided that R1 can also be hydrogen when X is --CO--; V is a divalent organic radical of 1 to 3 carbon atoms; n is 0, 1 or 2; R2 and R3 are the same or different and are each hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, vinyl, allyl, propenyl, cycloalkyl of 3 to 6 carbon atoms, cycloalkenyl of 3 to 6 carbon atoms, mono-, di- or tri-halo lower alkyl or aryl; R4, r5 and R6 are the same or different and are each hydrogen, nitro, cyano, (R)2 N--, (R)2 N--CO--, R--CO--NH--, R--O--CO--, R--CO--O--, R--, R--O--, wherein R is as above defined, H2 N--SO2 --, chlorine, bromine, iodine, fluorine or trifluoromethyl; G is hydrogen or straight or branched chain alkyl of 1 to 5 carbon atoms; and B is a moiety of the formula SPC6 wherein R7, r8 ad R9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--0--, R--S--, R--SO--, R--SO2 --, (R)2 N--, R--CO--NH--, or R--CO--O--, wherein R is as above defined; the arrow in the divalent linking group → means that the linkage of two atoms by the free valencies of his group must take place as indicated by the arrow; exhibit activity against both Gram-positive and Gram-negative bacteria.

Penicillins

Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the α-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamido or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.

Penicillins

Arylmethyl- and cyclohexenylmethyl- penicillins, substituted on the α-carbon atom of the side chain by a 2,3-disubstituted imidazolidinylcarbamide or a 2,3-disubstituted imidazolidinylthiocarbamido group, or by the corresponding 2,3-disubstituted 1,3-diazacyclohexylcarbamido or thiocarbamido groups are anti-bacterial agents.

Penicillins

Penicillins of the formula EQU1 or pharmaceutically acceptable non-toxic salts thereof, wherein C* is a carbon atom constituting a center of chirality; A is a moiety of the formula EQU2 or EQU3 wherein X is EQU4 Y is EQU5 or wherein Aryl is an aryl moiety; Z is EQU6 Q1 is EQU7 or SPC1 Q2 is EQU8 SPC2 or SPC3 R is straight- chain or branched alkyl of 1 to 5 carbon atoms; R1 is alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, alkenyl of 2 to 10 carbon atoms, cycloalkenyl of 3 to 10 carbon atoms. vinyl, arylvinyl, mono-, di-, or tri-halo-lower alkyl, H2 N--, R--NH--, (R)2 N--, aryl--NH--, aryl-lower alkylamino, alkoxy of 1 to 8 carbon atoms, aralkoxy of 1 to 8 carbon atoms in the alkoxy portion, cycloalkoxy of 3 to 7 carbon atoms, aryloxy, R--O--V--, R--S--V--, N=C--V--, R--O--CO--V--, H2 N--CO--V--, R--NH--CO--V--, R--O--CO--NH--, R--SO2 --NH--, (R)2 N--CO--V--, wherein R is as above defined, SPC4 SPC5 provided that when X is --SO2 --, R1 is not alkoxy, aralkoxy, cycloalkoxy or aryloxy, and further provided that R1 can also be hydrogen when X is --CO--; V is a divalent organic radical of 1 to 3 carbon atoms; n is 0, 1 or 2; R2 and R3 are the same or different and are each hydrogen, alkyl of 1 to 8 carbon atoms, alkenyl of 2 to 8 carbon atoms, vinyl, allyl, propenyl, cycloalkyl of 3 to 6 carbon atoms, cycloalkenyl of 3 to 6 carbon atoms, mono-, di- or tri-halo lower alkyl or aryl; R4, r5 and R6 are the same or different and are each hydrogen, nitro, cyano, (R)2 N--, (R)2 N--CO--, R--CO--NH--, R--O--CO--, R--CO--O--, R--, R--O--, wherein R is as above defined, H2 N--SO2 --, chlorine, bromine, iodine, fluorine or trifluoromethyl; G is hydrogen or straight or branched chain alkyl of 1 to 5 carbon atoms; and B is a moiety of the formula SPC6 wherein R7, r8 and R9 are the same or different and are each hydrogen, halogen, nitro, hydroxy, R--, R--O--, R--S--, R--SO-- , R--SO2 --, (R)2 N--, R--CO--NH--, or R--CO--O-- , wherein R is as above defined; the arrow in the divalent linking group ←Q2 → means that the linkage of two atoms by the free valencies of this group must take place as indicated by the arrow; exhibit activity against both Gram-positive and Gram-negative bacteria.