Abstract: The present invention provides a process for producing an amic acid ester represented by the following general formula (7) (wherein A is substituted or unsubstituted lower alkylene or the like; R1 is substituted or unsubstituted lower alkyl or the like; and R3 is hydrogen or lower alkyl), which process comprises reacting, in the presence of water, an amino acid represented by formula (1) with a halogenated carbonic acid ester represented by formula (2) (wherein X is halogen) to form an amide compound represented by formula (3), then reacting the amide compound with a halogenated carbonic acid ester represented by formula (4) (wherein R2 is substituted or unsubstituted lower alkyl or the like; and X is halogen) to form, in the system, a mixed acid anhydride represented by formula (5), and reacting the mixed acid anhydride with an amine compound represented by formula (6) (wherein Het is substituted or unsubstituted heterocyclic).

Abstract: According to the instant invention there have been found novel tetrazolinone derivatives represented by the general formula (I) wherein R1 represents methyl or ethyl, R2 represents halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, alkylsulfonyl, phenyl, phenoxy, alkoxycarbonyl, nitro or cyano, and n represents 0, 1, 2, 3, 4 or 5, processes and intermediates for their preparation and their use as herbicides.

Abstract: A method for producing a compound represented by the general formula (I-A) or the general formula (I-B), comprising the following step: wherein R1 is an optionally substituted lower alkyl, and the like; R2 is a lower alkyl or an optionally substituted aralkyl, and the like: R3 is a lower alkyl, characterized in that a compound represented by the general formula (II-A) or the general formula (II-B) is treated with thionyl chloride.

Abstract: The invention relates to p-thienylbenzylamides of formula (I) in which R(1), R(2), R(3), R(4), R(5), R(6) and X have the meanings given in the description. The compounds of formula (I) are potent agonists of angiotensin-(1-7) receptors and are useful as pharmaceutically active compounds to treat and/or prevent hypertension; cardiac hypertrophy; cardiac insufficiency; coronary heart diseases, such as angina pectoris; and endothelial dysfunction or endothelial damage as a consequence, for example, of atherosclerotic processes or in association with diabetes mellitus.

Abstract: Intermediates represented by the following formula: (wherein R1 is a hydrogen atom, an alkyl group, an aryl group, an aralkyl group or the like; X is a carboxyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aralkoxycarbonyl group, a formyl group, —CH2—Y, —CHZ1Z2, —CH(OR4)OR5 or the like), in the synthesis of biphenylamidine derivatives to be used as inhibitors for an activated blood coagulation factor X, and a process for preparing the same.

Abstract: Improved synthesis of seco(−)CBI (5-hydroxy-3-amino-1-[S]-(chloromethyl)-1,2 -dihydro-3H-benz(e)indole): and improved syntheses therefrom of a wide variety of CC-1065 analogs that comprise a cyclopropabenzidole (CBI) alkylating moiety, and which are collectively DC1 and its derivatives, for the synthesis of cell-targeted therapeutic agents.

Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

Abstract: Disclosed is a 6-acylamino-5-substituted-benzoxazol-2-one compound having the structural formula I: wherein Y is halogen or a substituent group linked to the rest of the compound by a hetero atom, and R′ is a group containing at least 8 carbon atoms. Also disclosed is a method for forming a cyan dye-forming coupler from the above compound. The method and intermediate provide a simplified manufacturing process.

Abstract: The invention relates to a new process for preparing a scopine ester useful as an intermediate in preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.

Abstract: Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

Abstract: The present invention relates to a method for producing a compound of the formula [71] wherein R1 is an optionally substituted cycloalkyl group, an optionally substituted aryl group or an optionally substituted heterocyclic group, R2 is a lower alkyl or a halogenated lower alkyl and R3 is a halogen atom or a hydrogen atom. The method of the present invention includes reacting compound [1] with thionyl chloride to give compound [2] and obtaining the objective compound [7] at a high yield via intermediate [5], and is utilizable for industrial production.

Abstract: The present invention relates to a photo-stabilizer of the general formula (I): wherein R1 is hydrogen, halogen, C1 to C12 alkyl, alkoxy (linear and branched), R2 is hydrogen, C1-C8 alkyl, cyclopentyl, cyclohexyl or cumyl, R3 is hydrogen, C1-C4 alkyl, R4 is methyl or ethyl, R5 is C1-C8 alkyl, alkyl phenyl, alkoxy, acyl, cycloalkyl and allyl, X is O, NH, C1-C8 alkyloxy and alkylamino (linear or branched), to derivatives and intermediates thereof.

Abstract: The invention relates to a new process for preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.

Abstract: This invention relates to a method for preparing 1-oxaspiro[2,5]-carbonitriles from ketones using spinning disc reactor technology.

Abstract: The present invention provides a process for producing an aziridine-1-carboxamide of the formula: from an aziridine of the formula: and an isocyanate of the formula R5—N═C═O, where R1, R2, R3, R4 and R5 are those defined herein. In addition, the present invention also provides a process for producing a 4-imino-1,3-diazabicyclo[3.1.0]-hexan-2-one of the formula: from the aziridine-1-carboxamide of Formula I.

Abstract: An improved process for the preparation of 5-(4-fluorophenyl)-1-[2-((2R,4R)-4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-ethyl]-2-isopropyl-4-phenyl-1H-pyrrole-3-carboxylic acid phenylamide by a novel synthesis is described where methyl cyanoacetate is converted in eight operations or fewer to the desired product, as well as other valuable intermediates used in the process.

Abstract: Compound of formula (I): wherein: R1, R2, R3, R4, R5, R6 and R8, which may be identical or different, each represents hydrogen, alkyl, arylalkyl, hydroxy, alkoxy, arylalkoxy, acyloxy, arylcarbonyloxy, carboxyalkyl or carboxy, R7 represents hydrogen, hydroxy, alkoxy, arylalkoxy, acyloxy or arylcarbonyloxy group, or one of R1 to R8, together with another of R1 to R8 adjacent to it, forms an alkylenedioxy, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid or base.

Abstract: Substituted pyranes such as 2-ethinyl-tetrahydro-2,6,6-trimethylpyran are prepared from dehydrolinalool or higher homologues thereof by heating or treatment with microwaves in the presence of a solid acid.

Abstract: The instant invention is a novel series of amino heterocycles useful in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, and sleep disorders. Processes for the preparation and intermediates useful in the preparation are also disclosed.