35166-36-0

Upstream product

• 16880-11-8 3-methoxyisoxazole-5-carboxylic acid methyl ester 
• 13626-59-0 3-methoxyisoxazole-5-carboxylic acid 
• 1026690-71-0 3-methoxyisoxazole-5-methanol THP ether 

Downstream Products

• 1053244-57-7 3-Methoxy-5-[2-((E)-2-methyl-3-{(2S,3S,4R,5S)-5-[(2S,3S)-3-((1R,2S)-1-methyl-2-trimethylsilanyloxy-propyl)-oxiranylmethyl]-3,4-bis-trimethylsilanyloxy-tetrahydro-pyran-2-yl}-propenyl)-4-(toluene-4-sulfonyl)-4,5-dihydro-oxazol-5-yl]-isoxazole 
• 143268-25-1 2-<(3-methoxy-5-isoxazolyl)methyl>-3-imino-6-phenyl-2,3-dihydropyridazine hydrochloride 
• 143268-27-3 2-<(3-methoxy-5-isoxazolyl)methyl>-3-imino-6-(p-chlorophenyl)-2,3-dihydropyridazine hydrochloride 
• 143268-28-4 2-<(3-methoxy-5-isoxazolyl)methyl>-3-imino-8-phenyl-2,3-dihydrobenzopyridazine hydrochloride 
• 100241-86-9 3-methoxy-5-(N-methyl-N-benzylaminoethyl)isoxazole 

Relevant academic research and scientific papers

THAILANSTATIN ANALOGS

The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins i

ISOXAZOLINE DERIVATIVES AND THEIR USE AS HERBICIDES

Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides. Also claimed is a process for the preparation of compounds of the formula I, wherein m is 2 and n is 1, and the other substituents are defined as in claim 1, formula (Ia) by reacting a compound of the formula Ia in a single step or stepwise in succession with compounds of the formula R5-X and/or R6-X, wherein R5 and R6 are as defined in claim 1, and X is a leaving group, and a process for the preparation of compounds of the formula I, wherein R6 is C1--C10alkyl or halogen, m is 2 and n is 1, and the other substituents are defined as in claim 1, formula (Ib) by reacting a compound of the formula 1b with a compound of the formula R5-X, wherein R5 is as defined in claim 1, and X is a leaving group, and a process for the preparation of compounds of the formula I, wherein R5 is chlorine, bromine or iodine, m is 1 or 2, and n is 1, and the other substituents are defined as in claim 1, formula (Ic) by reacting a compound of the formula le with an N- halosuccinimide and an oxidising agent.

MALONONITRILE COMPOUND AS PESTICIDES

The present invention provides a malononitrile compound represented by the formula (I): wherein any one of X1, X2, X3 and X4 is CR100, wherein R100 is a group represented by the formula: the other three of X1, X2, X3 and X4 each represent nitrogen or CR5, provided that 1 to 3 of X1, X2, X3 and X4 represent nitrogen, and Z represents oxygen, sulfur or NR6, which has pest-controlling activity.

Discovery of ritonavir, a potent inhibitor of HIV protease with high oral bioavailability and clinical efficacy

The structure-activity studies leading to the potent and clinically efficacious HIV protease inhibitor ritonavir are described. Beginning with the moderately potent and orally bioavailable inhibitor A-80987, systematic investigation of peripheral (P3 and P2') heterocyclic groups designed to decrease the rate of hepatic metabolism provided analogues with improved pharmacokinetic properties after oral dosing in rats. Replacement of pyridyl groups with thiazoles provided increased chemical stability toward oxidation while maintaining sufficient aqueous solubility for oral absorption. Optimization of hydrophobic interactions with the HIV protease active site produced ritonavir, with excellent in vitro potency (EC50 = 0.02 μM) and high and sustained plasma concentrations after oral administration in four species. Details of the discovery and preclinical development of ritonavir are described.

Structure-activity studies of 6-substituted decahydroisoquinoline-3- carboxylic acid AMPA receptor antagonists. 2. Effects of distal acid bioisosteric substitution, absolute stereochemical preferences, and in vivo activity

We have explored the excitatory amino acid antagonist activity in a series of decahydroisoquinoline-3-carboxyic acids, and within this series found the potent and selective AMPA antagonist (3SR,4aRS,6RS,8aRS)-6-(2-(1H-tetrazol- 5-yl)ethyl)decahydroisoquin

The chemistry of pseudomonic acid part 14. Synthesis and in vivo biological activity of heterocyclyl substituted oxazole derivatives

Semisynthetic analogues of pseudomonic acid A have been prepared containing a heterocyclyl substituted oxazole. Derivatives in which the heterocycle was thiophene, furan, pyridine, or isoxazole showed good antibacterial potency and were further evaluated in vivo. Both pharmacokinetic parameters and oral activity against an experimental intraperitoneal sepsis were superior to results obtained from previously described pseudomonic acid A derivatives.

Condensation of muscimol or thiomuscimol with aminopyridazines yields GABA-A antagonists

Ten analogs of muscimol and thiomuscimol in which the amino function was delocalized in an amidinic system were prepared by N2 alkylation of 6-aryl-3- aminopyridazines with (chloromethyl)isoxazole or (chloromethyl)isothiazole derivatives. These muscimol a

Process for the preparation of 3,5-disubstituted isoxazoles

A novel process for the preparation of 3-bromo- and 3-chloro-5-substituted isoxazoles is provided. Dibromo- or dichloro-formaldoxime is reacted with an excess of an 1-alkyne derivative of the formula where R is hydrogen, phenyl or 1-6 C alkyl optionally substituted by halogen, OH, OR', CHO, COR', COOR', CONH2, CONR'R" or NHCOR' where, in turn, R' and R", which may be the same or different, are a 1-6 C alkyl or haloalkyl, in the presence of (i) at least an equimolecular amount, with respect to the dibromo- or dichloro-formaldoxime, of an alkaline base selected from the class consisting of sodium and potassium carbonate and bicarbonate and (ii) an inert solvent in which the 1-alkyne is soluble at room temperature.