128346-20-3

Upstream product

• 34619-03-9 tert-butyldicarbonate 
• 68-41-7 cycloserine 
• 24424-99-5 di-tert-butyl dicarbonate 

Downstream Products

• 68-41-7 cycloserine 

Relevant academic research and scientific papers

Design and synthesis of 3-isoxazolidone derivatives as new Chlamydia trachomatis inhibitors

Chlamydia trachomatis (Ct) is a bacterial human pathogen responsible for the development of trachoma, the worldwide infection leading to blindness, and is also a major cause of sexually transmitted diseases. As iron is an essential metabolite for this bac

Cycloserine fatty acid derivatives as prodrugs: Synthesis, degradation and in Vitro skin permeability

Various 4,5-dihydroisoxazol-3-yl fatty acid ester derivatives of cycloserine were synthesized to improve skin permeation of cycloserine. The ester derivatives were prepared by using the tert-butoxycarbonyl (t-Boc) protection strategy. The 4,5-dihydroisoxazol-3-yl esters were readily hydrolysed in an aqueous buffer solution, and the degradation profiles showed both specific acid and specific base catalysis. In 50% human serum the formation of cycloserine was observed, but enzymatic catalysis was limited. Delivery through hairless mouse skin was investigated, and the apparent permeability coefficient was measured based on the flux of cycloserine into the receptor phase. The skin permeation of cycloserine across the hairless mouse skin was increased up to 20-fold by the fatty acid esters. The 4,5-dihydroisoxazol-3-yl fatty acid esters of cycloserine can therefore be considered as new topical prodrugs with the potential use in treatment of various skin infections.

Number selective NR2B antagonists

The present disclosure provides compounds of Formula (I) and pharmaceutically acceptable salts thereof. The Formula (I) compounds are ligands for NR2B N-Methyl-D-aspartate (NMD A) receptor and thereby making them useful for the treatment of various disord

ISOXAZOLINE DERIVATIVES AS INSECTICIDAL COMPOUNDS

The present invention provides compounds of formula I wherein G1 is oxygen; R1 is hydrogen; R2 is group P L is a bond, methylene or ethylene; R3 is hydrogen; R4 is independently hydrogen, cyano, cyano

Kinase inhibitor compounds

The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.

KINASE INHIBITOR COMPOUNDS

The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of kinase-mediated processes, and treatment of disease and disease symptoms, particularly those mediated by certain kinase enzymes.

Cyclic hydroxamates, especially multiply substituted [1,2]oxazinan-3-ones

Routes to putative N-acyl-D-ala-D-ala surrogates, beginning with the conversion of 4-, 5-, and 6-membered lactones into 5-, 6-, and 7-membered cyclic hydroxamates, are reported. The key step of the synthesis is trimethylaluminium-promoted cyclization of an ω-aminooxyester. The 7-membered cyclic hydroxamate crystallizes in a chair conformation. Extension of the reaction sequence to homoserine or homoserine lactone leads to cyclocanaline and N-acylated cyclocanalines. The 4-phenylacetamido derivative of cyclocanaline crystallizes in a boat conformation. The attachment of a 2-carboxypropyl substituent to the ring nitrogen of a 4-acylaminocyclocanaline has been effected, prior to cyclization, by coupling of the acyclic aminooxyester precursor to the triflate of benzyl lactate or, after cyclization, by coupling to tert-butyl α-bromopropionate in the presence of potassium fluoride - alumina, followed by removal of the protecting group in each case. A six-membered homolog of the antibiotic lactivicin has been synthesized by the reaction of 4-phenylacetamidocyclocanaline with benzyl 2-oxoglutarate in the presence of carbodiimide, followed by hydrogenolysis. Starting with methyl 2,4-dibromo-2,4-dideoxy-L-erythronate, which is available in two steps from L-ascorbic acid, these reaction sequences have been applied to the stereospecific synthesis of a D-alanine derivative whose nitrogen atom is enclosed within a 3,4-disubstituted [1,2]oxazinan-3-one.

SYNTHESIS OF AN AMINOISOXAZOLIDINE SUBSTITUTED QUINOLONE ACID

New heterocycle aminoisoxazolidine 7 and tetrafluorobenzoic acid are synthesized for the synthesis of a quinolone antibacterial agent.The synthesis of a chiral aminoisoxazolidine substituted quinolone acid, U-82662A, is described.