57772-82-4

Upstream product

• 6065-54-9 dimethyl dimethylmalonate 
• 100-39-0 benzyl bromide 
• 5659-93-8 2,2-Dimethylmalonyl chloride 
• 100-51-6 benzyl alcohol 
• 15014-25-2 malonic acid dibenzyl ester 
• 74-88-4 methyl iodide 
• 82794-36-3 dibenzyl methylmalonate 
• 595-46-0 2,2-dimethylmalonic acid 
• 122-60-1 Phenyl glycidyl ether 

Downstream Products

• 86507-74-6 3-(benzyloxy)-2,2-dimethyl-3-oxopropanoic acid 
• 813415-04-2 phenylmethyl 2-methyl-2-(2-propenyl)amidopropanoate 
• 813415-17-7 BnO-mAib-L-Ala-OH 
• 813415-16-6 BnO-mAib-L-Ala-OtBu 
• 123963-80-4 tetrabutylammonium benzyl 2,2-dimethylmalonate 

Relevant academic research and scientific papers

CHEMICAL COMPOUNDS

The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.

Total synthesis of sequential retro-peptide oligomers

The total synthesis of sequential oligomers of retro-peptides of the general formula Boc(-gGly-mAib)n-OBn, starting from dimethylmalonic acid, has been carried out in good overall yield. The key step is the formation of the gGly unit >N-CH

A Highly Regioselective Conversion of Epoxides to Halohydrins by Lithium Halides

Lithium halides in the presence of an acid (pKa 13) react with epoxides regioselectively to give vicinal halohydrins in high yields.The simplicity and convenience of this procedure makes it attractive for large scale synthesis.

Orally effective acid prodrugs of the β-lactamase inhibitor sulbactam

Sulbactam (1) is a β-lactamase inhibitor with limited oral bioavailability. Lipophilic double-ester prodrug sulbactam pivoxil (2) significantly improves the oral absorption of sulbactam, as does the mutual prodrug double ester sultamicillin (3). We have found that double-ester prodrugs of sulbactam terminating in a carboxyl group (8) also were effective oral-delivery vehicles in rats. Carboxyl-terminated double esters have several potential advantages over their nonionizable lipophilic counterparts, including water solubility, crystallinity, choice of salts for dosage forms, and formation of innocuous byproducts on hydrolysis.

Antibacterial 6'-(2-amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl penicillanate 1,1-dioxide compounds

6-(2-Amino-2-[4-acyloxyphenyl]acetamido)penicillanoyloxymethyl esters of penicillanic acid 1,1-dioxide are useful as antibacterial agents. Derivatives of the aforesaid antibacterial agents which have an amino protecting group on the amino function in the 2-amino-2-(4-acyloxyphenyl)acetamido side chain are useful intermediates to the antibacterial agents themselves.

1,1-Alkanediol dicarboxylate linked antibacterial agents

Useful antibacterial agents in which a penicillin and/or a beta-lactamase inhibitor are linked via 1,1-alkanediol dicarboxylates are of the formula STR1 where A is the residue of certain dicarboxyic acids, R3 is H or (C1 -C3), n is zero or 1 such that when n is zero R is P or B and R1 is the residue of certain esters, H or a salt thereof; and when n is 1, one of R and R1 is P and the other is B, and P is STR2 where R2 is H or certain acyl groups, and B is the residue of a beta-lactamase inhibiting carboxylic acid; a method for their use, pharmaceutical compositions thereof and intermediates useful in their production.

Cholestano-cobaloximes and Cholestano-rhodoximes. Synthesis, Characterisation, and Rearrangement of Model Compounds for the Active Site of Methylmalonyl-CoA Mutase

Cholestano-cobaloximes and cholestano-rhodoximes, three diastereoisomers of each constitution, were synthesised from cholestane-2,3-dione dioxime (3).The diastereoisomeric complexes were separated and characterised by their spectra.One of the axial ligands was invariably pyridine, the other either chlor (9), methyl (10), 2,2-bis(methoxycarbonyl)propyl (11), 2,2-bis(benzyloxycarbonyl)propyl (12), or 2,2-bis(2-naphthylmethoxycarbonyl)propyl (13 and 14).Irradiation of the complexes 11, 12, 13, and 14 in ethanol or 2-propanol afforded, apart from dimethylmalonic diester, other products among which was the corresponding methylsuccinic diester in yields of approx. 1, 20, 23, and 13percent, respectively.The methylsuccinic acid bis(2-naphthylmethyl ester) obtained from the irradiation of the diastereoisomeric cholestano-cobaloximes 13a, b and c was found to be practically racemic.