2,3-Bis(phenylsulfonyl)-1,3-butadiene as a Reagent for the Synthesis of the Azatricyclic Core (IX... more 2,3-Bis(phenylsulfonyl)-1,3-butadiene as a Reagent for the Synthesis of the Azatricyclic Core (IX) of (±)-Halichlorine. -Key steps are the stereoselective cycloaddition of the oxime (I) to the butadiene (II) and subsequent Na/Hg-mediated reduction giving the tricyclic piperidinone (V). -(FLICK, A.
Beim Erhitzen der Verbindung (II) in Benzol in Gegenwart von Mo(CO)6 entsteht das Produkt (I). Da... more Beim Erhitzen der Verbindung (II) in Benzol in Gegenwart von Mo(CO)6 entsteht das Produkt (I). Dagegen entsteht in Gegenwart des Komplexes Mo(CO)3L3 (L: Diglyme) in Benzol-Diglyme der Komplex (III). W ährend beim Erhitzen der Verbindung (V) in Benzol in Gegenwart des Komplexes Mo(CO)6 in Benzol der Komplex (IV) entsteht, f ührt die gleiche Reaktion in Toluol zum Produkt (VI). Die Kristallstruktur des Komplexes (III) wird bestimmt.
The dithioacetals (II), (IV), and (VIII) are coupled with the Grignard reagents (I) in the presen... more The dithioacetals (II), (IV), and (VIII) are coupled with the Grignard reagents (I) in the presence of Ni catalyst to give the (cyclo)alkenes (III), (V), (VI), (IX), and (XII). Isomers and dihydro derivatives such as (VII), (X), (XI), and (XIII) are also obtained. (Mechanism).
Synthesis of Novel Bicyclo[2.2.1] Ribonucleosides: 2'-Amino-and 2'-Thio-LNA Monomeric Nucleosides... more Synthesis of Novel Bicyclo[2.2.1] Ribonucleosides: 2'-Amino-and 2'-Thio-LNA Monomeric Nucleosides. -The formation of benzylated nucleosides (X) and (XII) is readily achieved by treatment of tosylates (III) with either benzylamine or potassium thioacetate.The thymidine derivative (X) is successfully debenzylated to afford the desired deprotected nucleoside (XI), whereas the direct debenzylation of the uridine derivative (XII) fails, probably due to catalyst poisoning. The deprotection of the tricyclic intermediate (VII), derived from nucleoside (IIIa), is thus the route of choice to obtain derivative (VIII). -(SINGH, S.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
In Gegenwart katalytischer Mengen an Palladiumchlorid (III), Triphenylphosphin (IV) und Natriumac... more In Gegenwart katalytischer Mengen an Palladiumchlorid (III), Triphenylphosphin (IV) und Natriumacetat (V) reagiert Phenylselenenyl-bromid (II) mit Ethylacrylat (I) in Benzonitril zu den jeweils zwei Phenylselenenylgruppen enthaltenden Kupplungsprodukten (VI) und (VII); ein Reaktionsmechanismus wird kurz diskutiert. Andere terminale Olefine reagieren ähnlich.
The dithioacetals (I) react with trimethylsilylmethylmagnesium chloride (II) in the presence of c... more The dithioacetals (I) react with trimethylsilylmethylmagnesium chloride (II) in the presence of catalytic amounts of a Ni(II) complex to yield selectively the E-vinylsilanes (III).
2,3-dibromo-1-(phenylsulfonyl)-1-propene as a versatile reagent for the synthesis of furans and c... more 2,3-dibromo-1-(phenylsulfonyl)-1-propene as a versatile reagent for the synthesis of furans and cyclopentenones: 2-methyl-4-[(phenyl-sulfonyl)methyl]furan and 2-methyl-3-[(phenylsulfonyl)methyl]-2-cyclopenten-1-one intermediate: 1-(phenylsulfonyl)-1,2-propadiene intermediate: 2,3-dibromo-1-(phenylsulfonyl)-1-propene product: 2-methyl-4-[(phenylsulfonyl)methyl]furan product: 2-methyl-3-[(phenylsulfonyl)methyl]-2-cyclopenten-1-one Keywords: addition, to CC; annulation, heterocyclic-[5]; cyclization, cycloaddition; cyclization, cycloaddition; oxidation, S SO2; oxidation, miscellaneous; rearrangements; dichloromethane (methylene chloride); methanol; triethylamine; bromine
Supplementary Material 2 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 2 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
Supplementary Material 3 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 3 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
L'invention concerne des composes de formule (I) ou un sel de ceux-ci ; dans laquelle R1, R2,... more L'invention concerne des composes de formule (I) ou un sel de ceux-ci ; dans laquelle R1, R2, R3, R4, R6, R8, R20, R30, Y, Z et n sont tels que definis dans la description. Des utilisations des composes comme medicaments, et dans la fabrication de medicaments pour le traitement d'une infection virale, en particulier une infection par le virus de l'hepatite C sont egalement decrites. L'invention comprend en outre des procedes de preparation de ces composes et formulations pharmaceutiques de ceux-ci.
La presente invention concerne des nouveaux composes, des compositions contenant lesdits composes... more La presente invention concerne des nouveaux composes, des compositions contenant lesdits composes et des methodes de traitement d'une infection virale, notamment, de l'hepatite C et du SARS. Plus specifiquement, cette invention a pour objet des composes macrocycliques contenant un aryle utilises dans l'inhibition de la replication virale du VHC et du SARS.
Supplementary Material 1 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 1 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
A compound of Formula I, or a pharmaceutically acceptable stereoisomer, tautomer or salt thereof,... more A compound of Formula I, or a pharmaceutically acceptable stereoisomer, tautomer or salt thereof, wherein, ** Formula ** X is N and Y is CR5, or Y is N and X is CR5; Z is N or CR6; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, cycloalkyl, substituted cycloalkyl, substituted heterocyclyl, aryloxy , substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, heterocyclyloxy, substituted heterocyclyloxy, cycloalkyloxy, substituted cycloalkyloxy, acyl, acylamino, acyloxy, amino, substituted amino, aminocarbonyl, aminothiocarbonyl, aminocarbonylamino, aminothiocarbonylamino, aminocarbonyloxy, aminosulfonyl, aminosulfonyloxy, aminosulfonylamino, amidino, carboxyl, carboxy ester, (carboxy ester) amino, (carboxy ester) oxy, cyano, halo, hydroxy, nitro, SO3H, sulfonyl, substituted sulfonyl, sulfo...
2,3-Bis(phenylsulfonyl)-1,3-butadiene as a Reagent for the Synthesis of the Azatricyclic Core (IX... more 2,3-Bis(phenylsulfonyl)-1,3-butadiene as a Reagent for the Synthesis of the Azatricyclic Core (IX) of (±)-Halichlorine. -Key steps are the stereoselective cycloaddition of the oxime (I) to the butadiene (II) and subsequent Na/Hg-mediated reduction giving the tricyclic piperidinone (V). -(FLICK, A.
Beim Erhitzen der Verbindung (II) in Benzol in Gegenwart von Mo(CO)6 entsteht das Produkt (I). Da... more Beim Erhitzen der Verbindung (II) in Benzol in Gegenwart von Mo(CO)6 entsteht das Produkt (I). Dagegen entsteht in Gegenwart des Komplexes Mo(CO)3L3 (L: Diglyme) in Benzol-Diglyme der Komplex (III). W ährend beim Erhitzen der Verbindung (V) in Benzol in Gegenwart des Komplexes Mo(CO)6 in Benzol der Komplex (IV) entsteht, f ührt die gleiche Reaktion in Toluol zum Produkt (VI). Die Kristallstruktur des Komplexes (III) wird bestimmt.
The dithioacetals (II), (IV), and (VIII) are coupled with the Grignard reagents (I) in the presen... more The dithioacetals (II), (IV), and (VIII) are coupled with the Grignard reagents (I) in the presence of Ni catalyst to give the (cyclo)alkenes (III), (V), (VI), (IX), and (XII). Isomers and dihydro derivatives such as (VII), (X), (XI), and (XIII) are also obtained. (Mechanism).
Synthesis of Novel Bicyclo[2.2.1] Ribonucleosides: 2'-Amino-and 2'-Thio-LNA Monomeric Nucleosides... more Synthesis of Novel Bicyclo[2.2.1] Ribonucleosides: 2'-Amino-and 2'-Thio-LNA Monomeric Nucleosides. -The formation of benzylated nucleosides (X) and (XII) is readily achieved by treatment of tosylates (III) with either benzylamine or potassium thioacetate.The thymidine derivative (X) is successfully debenzylated to afford the desired deprotected nucleoside (XI), whereas the direct debenzylation of the uridine derivative (XII) fails, probably due to catalyst poisoning. The deprotection of the tricyclic intermediate (VII), derived from nucleoside (IIIa), is thus the route of choice to obtain derivative (VIII). -(SINGH, S.
ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was e... more ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.
In Gegenwart katalytischer Mengen an Palladiumchlorid (III), Triphenylphosphin (IV) und Natriumac... more In Gegenwart katalytischer Mengen an Palladiumchlorid (III), Triphenylphosphin (IV) und Natriumacetat (V) reagiert Phenylselenenyl-bromid (II) mit Ethylacrylat (I) in Benzonitril zu den jeweils zwei Phenylselenenylgruppen enthaltenden Kupplungsprodukten (VI) und (VII); ein Reaktionsmechanismus wird kurz diskutiert. Andere terminale Olefine reagieren ähnlich.
The dithioacetals (I) react with trimethylsilylmethylmagnesium chloride (II) in the presence of c... more The dithioacetals (I) react with trimethylsilylmethylmagnesium chloride (II) in the presence of catalytic amounts of a Ni(II) complex to yield selectively the E-vinylsilanes (III).
2,3-dibromo-1-(phenylsulfonyl)-1-propene as a versatile reagent for the synthesis of furans and c... more 2,3-dibromo-1-(phenylsulfonyl)-1-propene as a versatile reagent for the synthesis of furans and cyclopentenones: 2-methyl-4-[(phenyl-sulfonyl)methyl]furan and 2-methyl-3-[(phenylsulfonyl)methyl]-2-cyclopenten-1-one intermediate: 1-(phenylsulfonyl)-1,2-propadiene intermediate: 2,3-dibromo-1-(phenylsulfonyl)-1-propene product: 2-methyl-4-[(phenylsulfonyl)methyl]furan product: 2-methyl-3-[(phenylsulfonyl)methyl]-2-cyclopenten-1-one Keywords: addition, to CC; annulation, heterocyclic-[5]; cyclization, cycloaddition; cyclization, cycloaddition; oxidation, S SO2; oxidation, miscellaneous; rearrangements; dichloromethane (methylene chloride); methanol; triethylamine; bromine
Supplementary Material 2 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 2 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
Supplementary Material 3 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 3 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
L'invention concerne des composes de formule (I) ou un sel de ceux-ci ; dans laquelle R1, R2,... more L'invention concerne des composes de formule (I) ou un sel de ceux-ci ; dans laquelle R1, R2, R3, R4, R6, R8, R20, R30, Y, Z et n sont tels que definis dans la description. Des utilisations des composes comme medicaments, et dans la fabrication de medicaments pour le traitement d'une infection virale, en particulier une infection par le virus de l'hepatite C sont egalement decrites. L'invention comprend en outre des procedes de preparation de ces composes et formulations pharmaceutiques de ceux-ci.
La presente invention concerne des nouveaux composes, des compositions contenant lesdits composes... more La presente invention concerne des nouveaux composes, des compositions contenant lesdits composes et des methodes de traitement d'une infection virale, notamment, de l'hepatite C et du SARS. Plus specifiquement, cette invention a pour objet des composes macrocycliques contenant un aryle utilises dans l'inhibition de la replication virale du VHC et du SARS.
Supplementary Material 1 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotox... more Supplementary Material 1 from CHIR-124, a Novel Potent Inhibitor of Chk1, Potentiates the Cytotoxicity of Topoisomerase I Poisons In vitro and In vivo
A compound of Formula I, or a pharmaceutically acceptable stereoisomer, tautomer or salt thereof,... more A compound of Formula I, or a pharmaceutically acceptable stereoisomer, tautomer or salt thereof, wherein, ** Formula ** X is N and Y is CR5, or Y is N and X is CR5; Z is N or CR6; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, alkoxy, substituted alkoxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclyl, cycloalkyl, substituted cycloalkyl, substituted heterocyclyl, aryloxy , substituted aryloxy, heteroaryloxy, substituted heteroaryloxy, heterocyclyloxy, substituted heterocyclyloxy, cycloalkyloxy, substituted cycloalkyloxy, acyl, acylamino, acyloxy, amino, substituted amino, aminocarbonyl, aminothiocarbonyl, aminocarbonylamino, aminothiocarbonylamino, aminocarbonyloxy, aminosulfonyl, aminosulfonyloxy, aminosulfonylamino, amidino, carboxyl, carboxy ester, (carboxy ester) amino, (carboxy ester) oxy, cyano, halo, hydroxy, nitro, SO3H, sulfonyl, substituted sulfonyl, sulfo...
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