Jim Tarrant | Harding University (original) (raw)
Papers by Jim Tarrant
ChemInform, Aug 17, 2010
www.cheminform.wiley-vch.de Benzopyran derivatives R 0350 A New Strategy for the Synthesis of 3-A... more www.cheminform.wiley-vch.de Benzopyran derivatives R 0350 A New Strategy for the Synthesis of 3-Acyl-Coumarin Using Mesoporous Molecular Sieve MCM-41 as a Novel and Efficient Catalyst.-A simple synthesis of 3-acyl-coumarins (III) via Knoevenagel condensation from 2-hydroxy-benzaldehydes (I) uses molecular sieves as a solid acid catalyst.-(HERAVI*, M. M.;
![Research paper thumbnail of New strategy for the synthesis of the taxane diterpenes: Formation of the BC-rings of taxol via a [5+2]-pyrylium ylide-alkene cyclization, ring expansion strategy](https://attachments.academia-assets.com/113206932/thumbnails/1.jpg)
](Tetrahedron Letters, Jul 1, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
Journal of the Chemical Society, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
Tetrahedron Letters, Jul 1, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharm... more The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.The invention claims compounds of formula I and the use of compounds of formula I or pharmaceutical salts thereof as oral drugs for the treatment of human or veterinary disease.in which:R is phenyl, isopropyl, or tert butyl;R is -C(O)R in which R is (CH3)3CO-, (CH3)3CCH2-, CH3(CH2)3O-, cyclobutyl-, cyclohexyloxy, or (2-furyl);R is CH3C(O)O-.
L'invention concerne des derives piperazine a substitution aryle, pouvant etre utilises pour ... more L'invention concerne des derives piperazine a substitution aryle, pouvant etre utilises pour moduler l'activite de recepteur MCH in vivo ou in vitro, et utiles en particulier dans le traitement de divers troubles metaboliques, de l'alimentation et sexuels, chez l'homme, les animaux domestiques et les animaux d'elevage. On decrit des compositions pharmaceutiques et des procedes permettant de traiter ces troubles, ainsi que des procedes d'utilisation de tels ligands pour la detection de recepteur MCH (par exemple, dans les etudes de localisation de recepteur).
La presente invention concerne des composes possedant la formule structurelle generale (I) et des... more La presente invention concerne des composes possedant la formule structurelle generale (I) et des derives pharmaceutiquement acceptables, tels que decrits generalement dans des classes et des sous-classes de cette invention. En outre, l'invention concerne des compositions pharmaceutiques associees, et leurs methodes d'utilisation dans le traitement d'un quelconque trouble ou d'une quelconque maladie parmi un certain nombre de troubles ou de maladies impliquant la fibrose et la proliferation cellulaire et ou l'activite antifibrotique ou antiproliferative est benefique.
The present invention provides compounds having the general structural formula (I) and pharmaceut... more The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
Des composes de Formule (I) sont proposes, dans lesquels des variables sont telles que decrites i... more Des composes de Formule (I) sont proposes, dans lesquels des variables sont telles que decrites ici. De tels composes peuvent etre utilises pour moduler une liaison MCH a des recepteurs MCH in vivo ou in vitro, et sont particulierement utiles dans le traitement de divers affections metaboliques, nutritives et sexuelles chez les humains, les animaux domestiques et les animaux d'elevage. Des compositions pharmaceutiques et des procedes pour traiter de telles affections sont proposes, comme les procedes pour utiliser de tels ligands pour detecter des recepteurs MCH (par exemple dans des etudes de localisation des recepteurs).
ChemInform, Aug 17, 2010
www.cheminform.wiley-vch.de Benzopyran derivatives R 0350 A New Strategy for the Synthesis of 3-A... more www.cheminform.wiley-vch.de Benzopyran derivatives R 0350 A New Strategy for the Synthesis of 3-Acyl-Coumarin Using Mesoporous Molecular Sieve MCM-41 as a Novel and Efficient Catalyst.-A simple synthesis of 3-acyl-coumarins (III) via Knoevenagel condensation from 2-hydroxy-benzaldehydes (I) uses molecular sieves as a solid acid catalyst.-(HERAVI*, M. M.;
Tetrahedron Letters, Jul 1, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
Journal of the Chemical Society, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
Tetrahedron Letters, Jul 1, 1995
Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered... more Solvolysis of the neopentyl triflates 14,25 and 32 resulted in ring expansion of a seven-membered ring into the eight-membered ring required for the synthesis of the taxanes diterpenoids, Our previous papers have focused on the reductive cleavage of an internal cyclopropane bond (C-l/C-11) to construct the eight-membered Bring of the taxanes. 1 An alternative approach that still utilizes the bicyclo[5.4.0]undecenones 3 (X = OTBS and X = H) is shown in Scheme 1. Conjugate addition of a methyl group to 3 leads to 2, which upon suitable activation of the C-10 alcohol and ionization (solvolysis), has the potential to undergo a semi-pinacol-type rearrangement to give 1.2 In this paper we report the implementation of this strategy. Fir '0 KOR 1 Ring expansion in the,top-half // 14 " 20 Taxane numbering \OR 3 Scheme 1 Ring expansion strategy (X = OTBS or H); TBS = ButMe2Si Me ?r2OMoM Lo5QoTBs 5 CHO ' H : Me'
The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharm... more The present invention concerns novel taxane derivatives, their use as antitumor agents, and pharmaceutical formulations.The invention claims compounds of formula I and the use of compounds of formula I or pharmaceutical salts thereof as oral drugs for the treatment of human or veterinary disease.in which:R is phenyl, isopropyl, or tert butyl;R is -C(O)R in which R is (CH3)3CO-, (CH3)3CCH2-, CH3(CH2)3O-, cyclobutyl-, cyclohexyloxy, or (2-furyl);R is CH3C(O)O-.
L'invention concerne des derives piperazine a substitution aryle, pouvant etre utilises pour ... more L'invention concerne des derives piperazine a substitution aryle, pouvant etre utilises pour moduler l'activite de recepteur MCH in vivo ou in vitro, et utiles en particulier dans le traitement de divers troubles metaboliques, de l'alimentation et sexuels, chez l'homme, les animaux domestiques et les animaux d'elevage. On decrit des compositions pharmaceutiques et des procedes permettant de traiter ces troubles, ainsi que des procedes d'utilisation de tels ligands pour la detection de recepteur MCH (par exemple, dans les etudes de localisation de recepteur).
La presente invention concerne des composes possedant la formule structurelle generale (I) et des... more La presente invention concerne des composes possedant la formule structurelle generale (I) et des derives pharmaceutiquement acceptables, tels que decrits generalement dans des classes et des sous-classes de cette invention. En outre, l'invention concerne des compositions pharmaceutiques associees, et leurs methodes d'utilisation dans le traitement d'un quelconque trouble ou d'une quelconque maladie parmi un certain nombre de troubles ou de maladies impliquant la fibrose et la proliferation cellulaire et ou l'activite antifibrotique ou antiproliferative est benefique.
The present invention provides compounds having the general structural formula (I) and pharmaceut... more The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.
Des composes de Formule (I) sont proposes, dans lesquels des variables sont telles que decrites i... more Des composes de Formule (I) sont proposes, dans lesquels des variables sont telles que decrites ici. De tels composes peuvent etre utilises pour moduler une liaison MCH a des recepteurs MCH in vivo ou in vitro, et sont particulierement utiles dans le traitement de divers affections metaboliques, nutritives et sexuelles chez les humains, les animaux domestiques et les animaux d'elevage. Des compositions pharmaceutiques et des procedes pour traiter de telles affections sont proposes, comme les procedes pour utiliser de tels ligands pour detecter des recepteurs MCH (par exemple dans des etudes de localisation des recepteurs).