摘要:
Sulfonamide-containing hydroxyethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要:
The invention relates to an enzymatic process for the stereoselective preparation of a hetero-bicyclic alcohol enantiomer, characterized in that a substantially pure enantiomer of the general formula ##STR1## wherein X is O, S, NH, N--(C.sub.1 -C.sub.4)alkyl or CH.sub.2 ; Y.sub.1, Y.sub.2 and Y.sub.3 are each independently hydrogen or substituents selected from halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 haloalkyl, nitro and cyano;the NO.sub.2 substituent is attached to the bicyclic ring system in the 5- or 7-position; andthe C*-atom has either the R or the S configuration;is prepared from its corresponding alcohol racemate by the following successive reaction steps:(1) stereoselective esterification,(2) separation of the alcohol from the ester produced,(3) hydrolysis of the ester to produce the corresponding alcohol enantiomer, and(4) conversion of the alcohol enantiomer into the starting racemate under basic conditions in order to allow its reuse.The invention also relates to a substantially pure alcohol enantiomer of formula I, to the use of the enantiomer for the preparation of a pharmacologically active piperazine derivative, and to substantially pure enantiomeric intermediates.
摘要:
Sulfonamide-containing hydroxethylamine compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
摘要:
Compounds of the formula I ##STR1## wherein X, Y and v are as defined below, novel intermediates used in their synthesis, and the pharmaceutically acceptable salts of such compounds and intermediates. The compounds of formula I and the novel intermediates used in their synthesis are muscarinic receptor antagonists that are selected for smooth muscle muscarinic sites and are useful in the prevention and treatment of diseases associated with altered motility or tone of smooth muscle, such as irritable bowel syndrome, diverticular disease, urinary incontinence, aesophageal achalasia, and chronic obstructive airways disease.
摘要:
A process for the production of substituted vinylbenzenes of the general formula: ##STR1## wherein R is a lower alkyl group having 1 to 4 C atoms, R.sub.1 is hydrogen or an acetyl group and R.sub.2 is hydrogen, a lower alkyl group having 1 to 4 C atoms or a benzyl group. A trialkylhydroquinone is cyclized with an aldehyde to an acetal and the latter is pyrolized to the endproduct. The substituted vinylbenzenes are valuable intermediate products in the synthesis of antioxidants.
摘要:
Fungicidal and plant growth-regulating hydroxyalkylazolyl derivatives of the formula ##STR1## in which R represents hydrogen, alkyl or acyl,R.sup.1 represents halogen, optionally substituted phenyl or the grouping --Z--R.sup.3, whereinZ represents oxygen, sulphur, SO or SO.sub.2 andR.sup.3 represents optionally substituted alkyl, optionally substituted phenyl or optionally substituted phenylalkyl,R.sup.2 represents optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted naphthyl or the radical of the formula ##STR2## m represents the numbers, 0, 1, 2 or 3, or R.sup.2 represents the radical or the formula ##STR3## X represents nitrogen or a CH group and Y represents the groupings --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, ##STR4## and their addition products with acids and metal salts. Intermediates of the formulas ##STR5## are also new.
摘要:
1,4-Benzodioxane derivatives represented by the following general formula: ##STR1## wherein p stands for an integer of 0-2, X and Y are same or different, and each represent a hydrogen atom; or a group represented by the formula --OR in which R denotes a hydrogen atom, a lower alkyl, lower alkoxycarbonyl or acyl group, or a group represented by the formula ##STR2## m being an integer of 1 or 2; cyano group; or carboxy group, n is an integer of 1-3, exclusive of the case wherein p=0 and X=Y=H, or a pharmacologically acceptable salt thereof. Their process for the preparation, their use as therapeutic and/or preventive compositions for ischemic heart diseases and heart failure and their application for the control of blood pressure during surgical operations are also described.
摘要:
Compounds of the forulae I and Ia ##STR1## in which R.sup.1 is a group which can be transferred to carbonyl or imine compounds, for example alkyl, allyl, vinyl or the radical of an enol or enamine, R.sup.2 is, for example, cyclopentadienyl, R.sup.3 is the radical of an optically active sugar or sugar derivative, Me is Ti, Zr or Hf, x is 0, 1 or 2 and y is 0, 1, 2 or 3, M.sym. is Li.sym., Na.sym., K.sym., MgY.sym., ZnY.sym., CdY.sym., HgY, CuY.sym. or quaternary ammonium, Y being halogen, are suitable for use as chiral reactants for compounds containing aldehyde, keto and/or N-substituted imine groups.
摘要:
The invention is insecticidal diaminoguanidine hydrazone compounds which are also effective antifeeding agents for insects and methods for their preparation.