Banyu Pharmaceutical Co. Ltd

Merck + Co., Inc.

Other

Banyu Pharmaceutical Coaltd

Toshiaki Mase

Toshio Nagase

Masaki Ihara

Kiyofumi Ishikawa

Mitsuo Yano

Takehiro Fukami

Takashi Hayama

Kenji Niiyama

Kagari Fujita

Masaru Nishikibe

Fumihiko Ikemoto

Takehiko Iida

Ralph P Volante

David M Tschaen

Kenji Maeda

Steven A Weissman

Kenichi Asakawa

Hiroki Sato

Matthew Heileman

Akio Kanatani

Masashi Kawasaki

Shinji Kato

Morihiro Mitsuya

Toshihiro Wada

Fumio Nakano

Yoshimi Tsuchiya

Takahiro Fukuroda

Ioannis N Houpis

Takahiro Itoh

Kazuhito Noguchi

Ilias K Dorziotis

Kensuke Kobayashi

Shouichi Hiraga

Asayuki Kamatani

Fengrui Lang

Masayuki Hagiwara

Takeshi Hayama

Disclosed is an efficient and widely-applicable method for commercially producing a thioether compound or a thiol compound which is useful as a pharmaceutical compound or a production intermediate of it. Specifically disclosed is a method for producing a thioether compound represented by the general formula [I] below or a salt thereof. This method is characterized in that a compound represented by the following general formula [III]: [III] (wherein X represents a bromine atom, a chlorine atom or a trifluoromethylsulfonyloxy group, and ring A represents an aryl group or a heteroaryl ring group) or a salt thereof is reacted with a thiol compound represented by the following general formula [II]: [II] or a salt thereof in the presence of a palladium compound such as Pd(dba), a base such as i-PrNEt and a phosphorus compound represented by the following formula [AA].

Method for producing thioether compound

This invention relates to a process for making spirolactone compounds analogous to formula I. 

Process for making spirolactone compounds

A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group. Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R&#x2014;Mg&#x2014;X (I) (wherein Rrepresents a halogen atom or an optionally substituted hydrocarbon residue; and Xrepresents a halogen atom) and an organolithium compound represented by the formula R&#x2014;Li (II)(wherein Rrepresents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.

Process for exchanging functional groups by halogen-metal exchange reaction

This invention relates to a process for making spirolactone compounds analogous to formula I 

A method by which a halogen atom of a halogen compound can be efficiently replaced with an electrophilic group. Also provided are: a reagent for converting a functional group through a halogen-metal exchange reaction, characterized by comprising either a mixture of a magnesium compound represented by the formula R&#x2014;Mg&#x2014;X (I) (wherein Rrepresents a halogen atom or an optionally substituted hydrocarbon residue; and Xrepresents a halogen atom) and an organolithium compound represented by the formula R&#x2014;Li (II) (wherein Rrepresents an optionally substituted hydrocarbon residue) or a product of the reaction of the magnesium compound with the organolithium compound; and a process for producing with the reagent a compound in which a halogen atom of a halogen compound has been replaced with an electrophilic group.

Method of converting functional group through halogen-metal exchange reaction

A process for preparing indolopyrrolocarbazole derivatives &lsqb;I&rsqb; by trating a compound &lsqb;V&rsqb; with a base in an inert solvent to prepare a compound &lsqb;IV&rsqb;, reacting the compound &lsqb;IV&rsqb; with a compound &lsqb;III&rsqb;to prepare a compound &lsqb;II&rsqb;, and deblocking the compound &lsqb;II&rsqb;; intermediates &lsqb;II&rsqb;, &lsqb;III&rsqb; and &lsqb;IV&rsqb;; and a process for preparing compounds &lsqb;III&rsqb;: &lsqb;wherein Y is hydrogen, C alkyl, phenyl, benzyloxymethyl, or aralkyl; R , R , R , R , R , and R are each independently a hydroxyl-protecting group; R and R are each independently hydrogen or a hydroxyl-protecting group; and X is an acid molecule&rsqb;. The above process is a safe and easy industrial process for preparing indolopyrrolocarbazole derivatives &lsqb;1&rsqb; useful as antitumor agents.

Process for preparing indolopyrrolocarbazole derivatives, intermediates therefor, and preparation process of the intermediates

Michael addition conducted in the presence of a zinc-amine complex and additional amounts of the amine component results in product with high diastereomeric excess.

Diastereoselective preparation of Michael adducts

Substituted piperidine derivatives as muscarinic M.sub.3 receptor

Aminopyridine derivatives

Endothelin antagonistic heteroaromatic ring-fused cyclopentene

The invention relates to compounds which are antagonists of endothelin, to processes for their preparation, and to their use as pharmaceuticals. The compounds of the invention are Useful in the treatment of hypertension, pulmonary hypertension, Reynaud's disease, myocardial infarction, angina pectoris, acute renal failure, cerebral infarction, cerebral vasospasm, arteriosclerosis, asthma, endotoxin shock, endotoxin-induced multiple organ failure or disseminated intravascular coagulation, and/or cyclosporin-induced renal failure or hypertension.

Endothelin antagonistic peptide derivatives

Peptides having the formula: ##STR1## inhibit the binding of endothelin to its ET.sub.B receptor and are useful in treating diseases associated with excess production or secretion of endothelin.

Endothelin antagonistic substance

Peptides having the formula: ##STR1## inhibit the binding of endothelin and are useful in treating diseases associated with excess production or secretion of endothelin.

Peptides having the formula: ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.

Peptides having the formula ##STR1## inhibit the binding of endothelin to its receptor and are useful in treating diseases associated with excess production or secretion of endothelin.

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Tsukuba, Japan

Toshiaki Mase