17 research outputs found
(2R)-4-[(9H-Fluoren-9-ylmethÂoxy)carbonÂyl]-2-methylÂpiperazin-1-ium chloride
The synthesis of the title salt, C20H23N2O2
+·Cl−, was carried out with a precursor of known absolute configuration (R) and the X-ray analysis confirmed that the product retained the absolute configuration. In the crystal, the dominant packing motif is a chain running along [010] generated by N—H⋯Cl hydrogen bonding. C—H⋯O and C—H⋯Cl interÂactions are also observed
From N-nitroacetylproline to leucylproline
The potential of the nitroacetyl group in peptide synthesis has been demonstrated by converting N-nitroacetylproline ethyl ester into cyclo(L-Leu-L-Pro)
Nitroacetyl group as a peptide synthon: synthesis of dipeptides with an α,α-bisallylglycine residue at the N-terminus
N-Nitroacetyl derivatives of L-proline, L-valine, and L-phenylalanine esters were prepared in two steps under mild conditions (Scheme 2). Regiospecific mono- and bis-allylation of these nitroacetyl derivatives were accomplished in presence of a Pd(0) catalyst. The bis-allyl derivatives 7-9 were obtained in 40-75% yield. The tertiary NO<SUB>2</SUB> group in these compounds could be transformed into an acetylamino group by Zn/AcOH/Ac<SUB>2</SUB>O. The final products 11-13 are dipeptides in which the N-terminal glycine residue bears two α-allyl substituents
Nitroketene-s, n-acetals as precursors for nitroacetamides and the elusive nitrothioacetahides
1-Amino-1-methylthio-2-nitroethenes (2) can be converted in high yields to the Nitroacetamides (3) by Hg<SUP>2+</SUP> catalysed hydrolysis and to the Nitrothioacetamides (4) by Na<SUB>2</SUB>S in ethanol-acetic acid
Is the nitro group attracted towards sulphur?
Evidence is presented for a significant, orientation sensitive, attractive intramolecular interaction between sulphur and a nitro group
Polymorphs and Cocrystals of Nalidixic Acid
Only one X-ray crystal structure of the parent quinolone
antibiotic nalidixic acid is known in the published and patent literature.
A systematic search for new solid-state forms of the drug yielded
two polymorphs (forms II and III) and six cocrystals with resorcinol,
catechol, hydroquinone, pyrogallol, orcinol, and phloroglucinol. Of
these, X-ray crystal structures were determined for polymorph II and
cocrystals with resorcinol, catechol, hydroquinone, and pyrogallol,
whereas the remaining solid forms were identified by their unique
powder X-ray diffraction patterns. Nalidixic acid is intramolecularly
O–H···O hydrogen bonded in a six-member ring,
and its molecular dimers are assembled via C–H···O
synthon. The OH donors on phenolic coformers H bond with the α-keto
acid moiety of the drug as connectors and spacers. Intermolecular
drug–drug C–H···O interactions in polymorphs
are replaced by strong drug–coformer O–H···O
hydrogen bonds in cocrystals
Polymorphs and Cocrystals of Nalidixic Acid
Only one X-ray crystal structure of the parent quinolone
antibiotic nalidixic acid is known in the published and patent literature.
A systematic search for new solid-state forms of the drug yielded
two polymorphs (forms II and III) and six cocrystals with resorcinol,
catechol, hydroquinone, pyrogallol, orcinol, and phloroglucinol. Of
these, X-ray crystal structures were determined for polymorph II and
cocrystals with resorcinol, catechol, hydroquinone, and pyrogallol,
whereas the remaining solid forms were identified by their unique
powder X-ray diffraction patterns. Nalidixic acid is intramolecularly
O–H···O hydrogen bonded in a six-member ring,
and its molecular dimers are assembled via C–H···O
synthon. The OH donors on phenolic coformers H bond with the α-keto
acid moiety of the drug as connectors and spacers. Intermolecular
drug–drug C–H···O interactions in polymorphs
are replaced by strong drug–coformer O–H···O
hydrogen bonds in cocrystals
Polymorphs and Cocrystals of Nalidixic Acid
Only one X-ray crystal structure of the parent quinolone
antibiotic nalidixic acid is known in the published and patent literature.
A systematic search for new solid-state forms of the drug yielded
two polymorphs (forms II and III) and six cocrystals with resorcinol,
catechol, hydroquinone, pyrogallol, orcinol, and phloroglucinol. Of
these, X-ray crystal structures were determined for polymorph II and
cocrystals with resorcinol, catechol, hydroquinone, and pyrogallol,
whereas the remaining solid forms were identified by their unique
powder X-ray diffraction patterns. Nalidixic acid is intramolecularly
O–H···O hydrogen bonded in a six-member ring,
and its molecular dimers are assembled via C–H···O
synthon. The OH donors on phenolic coformers H bond with the α-keto
acid moiety of the drug as connectors and spacers. Intermolecular
drug–drug C–H···O interactions in polymorphs
are replaced by strong drug–coformer O–H···O
hydrogen bonds in cocrystals
Polymorphs and Cocrystals of Nalidixic Acid
Only one X-ray crystal structure of the parent quinolone
antibiotic nalidixic acid is known in the published and patent literature.
A systematic search for new solid-state forms of the drug yielded
two polymorphs (forms II and III) and six cocrystals with resorcinol,
catechol, hydroquinone, pyrogallol, orcinol, and phloroglucinol. Of
these, X-ray crystal structures were determined for polymorph II and
cocrystals with resorcinol, catechol, hydroquinone, and pyrogallol,
whereas the remaining solid forms were identified by their unique
powder X-ray diffraction patterns. Nalidixic acid is intramolecularly
O–H···O hydrogen bonded in a six-member ring,
and its molecular dimers are assembled via C–H···O
synthon. The OH donors on phenolic coformers H bond with the α-keto
acid moiety of the drug as connectors and spacers. Intermolecular
drug–drug C–H···O interactions in polymorphs
are replaced by strong drug–coformer O–H···O
hydrogen bonds in cocrystals