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Molecules, Volume 3, Issue 1 (January 1998), Pages 1-30, Articles M43-M45

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Research

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Open AccessArticle Synthesis and Intramolecular [4+2] Cycloaddition Reactions of 4-Pyridazinecarbonitriles with Alkyne Side Chains
Molecules 1998, 3(1), 10-15; doi:10.3390/30100010
Received: 15 October 1997 / Accepted: 19 November 1997 / Published: 25 January 1998
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Abstract
The preparation of a series of new 3-(alkynyl-X)-substituted 4-pyridazinecarbonitriles 2-5 (X = O, NH) is described. The compounds are shown to undergo thermally induced intramolecular Diels-Alder reactions with inverse electron demand, affording the fused benzonitriles 6-8. Incorporation of a 1,2-phenylene unit into the
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The preparation of a series of new 3-(alkynyl-X)-substituted 4-pyridazinecarbonitriles 2-5 (X = O, NH) is described. The compounds are shown to undergo thermally induced intramolecular Diels-Alder reactions with inverse electron demand, affording the fused benzonitriles 6-8. Incorporation of a 1,2-phenylene unit into the side chain, as in the case of compounds 10 and 13, results in a more favorable conformation of the dienophilic substructure and thus to a pronounced acceleration of the [4+2] cycloaddition reaction. Full article
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Open AccessArticle Synthesis and Biological Evaluation of 14 -Methoxy Digitalis Derivatives
Molecules 1998, 3(1), 20-25; doi:10.3390/30100020
Received: 11 November 1997 / Accepted: 15 January 1998 / Published: 25 January 1998
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Abstract
The synthesis and biological evaluation of 14β-methoxy derivatives of digitoxigenin and of other digitalis-like compounds are reported. These compounds have a 14β-oxygen, which can be a hydrogen bonding acceptor, as is the case of 14β,15β-epoxide derivatives, but not a hydrogen bonding donor as
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The synthesis and biological evaluation of 14β-methoxy derivatives of digitoxigenin and of other digitalis-like compounds are reported. These compounds have a 14β-oxygen, which can be a hydrogen bonding acceptor, as is the case of 14β,15β-epoxide derivatives, but not a hydrogen bonding donor as is the case of 14β-hydroxy derivatives. All the new 14β-methoxy derivatives show a considerable reduced binding affinity on Na+,K+-ATPase when compared with the 14β-hydroxy analogues and also with the 14β,15β-epoxy derivatives. These results could mean that the digitalis receptor does not permit the presence of a bulky substituent in the 14β region, even of relatively small volume like the methyl group Full article
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Open AccessCommunication Nucleophilic Additions of 2-Furyllithium to Carbonyl Derivatives of L-Serine. Formal Synthesis of (2R,3R)-β-Hydroxy Aspartic Acid
Molecules 1998, 3(1), 26-30; doi:10.3390/30100026
Received: 1 October 1997 / Accepted: 15 January 1998 / Published: 25 January 1998
Cited by 2 | PDF Full-text (28 KB) | HTML Full-text | XML Full-text
Abstract
The nucleophilic addition of 2-furyllithium to esters derived from L-serine is described. The obtained furyl ketone 5 is stereoselectively reduced (ds≥95%) with sodium borohydride to afford the corresponding syn aminoalcohol 12 in enantiomerically pure form. Compound 12 was further converted into valuable α-hydroxy-β-amino
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The nucleophilic addition of 2-furyllithium to esters derived from L-serine is described. The obtained furyl ketone 5 is stereoselectively reduced (ds≥95%) with sodium borohydride to afford the corresponding syn aminoalcohol 12 in enantiomerically pure form. Compound 12 was further converted into valuable α-hydroxy-β-amino acids by means of the furan-to-acid equivalence. Full article
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Review

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Open AccessReview 4-Aryldihydropyrimidines via the Biginelli Condensation: Aza-Analogs of Nifedipine-Type Calcium Channel Modulators
Molecules 1998, 3(1), 1-9; doi:10.3390/30100001
Received: 29 October 1997 / Accepted: 8 December 1997 / Published: 25 January 1998
Cited by 85 | PDF Full-text (272 KB) | HTML Full-text | XML Full-text
Abstract Recent results from the author's laboratory in the area of dihydropyrimidine chemistry are summarized. Full article
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Open AccessReview Review of the Molecule of the Month Website in 1997
Molecules 1998, 3(1), 16-19; doi:10.3390/30100016
Received: 12 December 1997 / Accepted: 14 January 1998 / Published: 25 January 1999
Cited by 2 | PDF Full-text (136 KB) | HTML Full-text | XML Full-text
Abstract This review describes the history of the "Molecule of the Month" Website, along with a short summary of some of the molecules which featured during 1997. Full article
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Other

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Open AccessShort Note 3-Bis(5-methylfur-2-yl)methyl-2,4-pentanedion
Molecules 1998, 3(1), M43; doi:10.3390/M43
Received: 22 December 1997 / Published: 25 January 1998
PDF Full-text (96 KB) | Supplementary Files
(This article belongs to the Section Molbank Section of Molecules, 1997-2001)
Open AccessShort Note 2-Cyanophenylbis(5-methylfur-2-yl)methane
Molecules 1998, 3(1), M44; doi:10.3390/M44
Received: 22 December 1997 / Published: 25 January 1998
PDF Full-text (76 KB) | Supplementary Files
(This article belongs to the Section Molbank Section of Molecules, 1997-2001)
Open AccessShort Note a,a,a',a'- Tetra(5-methylfur-2-yl)-p-xylene
Molecules 1998, 3(1), M45; doi:10.3390/M45
Received: 22 December 1997 / Published: 25 January 1998
PDF Full-text (85 KB) | Supplementary Files
(This article belongs to the Section Molbank Section of Molecules, 1997-2001)

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