Jola Jas | Cracow University of Technology (original) (raw)
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Papers by Jola Jas
Archiv der Pharmazie, 2012
The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, bu... more The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, buspirone 1b, and NAN-190 1c.
Journal of Heterocyclic Chemistry, 2008
N-Alkylation of imides in the reaction of imides and alkylhalides, catalyzed by PT catalysts unde... more N-Alkylation of imides in the reaction of imides and alkylhalides, catalyzed by PT catalysts under solvent-free conditions, has been developed. The reaction occurs in the presence of K 2 CO 3 , and in many cases it takes place spontaneously. In the N-benzylation reaction, it has been recognized that TBAB (tetrabutylammonium bromide) and TBATFB (tetrabutylammonium tetrafluoroborate) show highest catalytic effect. Versatility and synthetic capacity of the solvent-free alkylation has been confirmed by Nbenzylation and N-ethylation of various imides. The developed procedure gives easy access to N-(bromoalkyl)imides.
…, 2011
The synthesis and evaluation as 5-HT 1A and 5-HT 7 serotonin receptor ligands of the two sets of ... more The synthesis and evaluation as 5-HT 1A and 5-HT 7 serotonin receptor ligands of the two sets of O-substituted hydroxybenzamides, structurally related to 2-{3-[4-(2-methoxyphenyl)piperazin-1-yl]pro-poxy}benzamide (1), (K i 5-HT 1A ¼ 21 nM, 5-HT 7 ¼ 234 nM) are reported. To affect the affinity for 5-HT 1A and 5-HT 7 receptors, an amide moiety (2-6) and a hydrocarbon chain length (7-10) were modified. The serotonergic activity of compounds 2-10 was generally higher in the case of 5-HT 1A receptors compared with 5-HT 7 ones; the most active 5-HT 1A ligands being meta-isomer 2 (K i ¼ 7 nM) and both analogs of 1 with the longest spacer, i.e., penta-and hexa-methylene derivatives 9 and 10 (K i ¼ 4 and 3 nM, respectively). The observed biological properties of compounds 1-10 were elucidated using molecular modeling procedures. J. Heterocyclic Chem., 48, 192 (2011).
Archiv der Pharmazie, 2012
The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, bu... more The reductive alkylation of amines procedure was applied for the synthesis of aripiprazole 1a, buspirone 1b, and NAN-190 1c.
Journal of Heterocyclic Chemistry, 2008
N-Alkylation of imides in the reaction of imides and alkylhalides, catalyzed by PT catalysts unde... more N-Alkylation of imides in the reaction of imides and alkylhalides, catalyzed by PT catalysts under solvent-free conditions, has been developed. The reaction occurs in the presence of K 2 CO 3 , and in many cases it takes place spontaneously. In the N-benzylation reaction, it has been recognized that TBAB (tetrabutylammonium bromide) and TBATFB (tetrabutylammonium tetrafluoroborate) show highest catalytic effect. Versatility and synthetic capacity of the solvent-free alkylation has been confirmed by Nbenzylation and N-ethylation of various imides. The developed procedure gives easy access to N-(bromoalkyl)imides.
…, 2011
The synthesis and evaluation as 5-HT 1A and 5-HT 7 serotonin receptor ligands of the two sets of ... more The synthesis and evaluation as 5-HT 1A and 5-HT 7 serotonin receptor ligands of the two sets of O-substituted hydroxybenzamides, structurally related to 2-{3-[4-(2-methoxyphenyl)piperazin-1-yl]pro-poxy}benzamide (1), (K i 5-HT 1A ¼ 21 nM, 5-HT 7 ¼ 234 nM) are reported. To affect the affinity for 5-HT 1A and 5-HT 7 receptors, an amide moiety (2-6) and a hydrocarbon chain length (7-10) were modified. The serotonergic activity of compounds 2-10 was generally higher in the case of 5-HT 1A receptors compared with 5-HT 7 ones; the most active 5-HT 1A ligands being meta-isomer 2 (K i ¼ 7 nM) and both analogs of 1 with the longest spacer, i.e., penta-and hexa-methylene derivatives 9 and 10 (K i ¼ 4 and 3 nM, respectively). The observed biological properties of compounds 1-10 were elucidated using molecular modeling procedures. J. Heterocyclic Chem., 48, 192 (2011).