- 1-HYDROXYCYCLOPROPANECARBOXALDEHYDE TETRAHYDROPYRANYL ETHER. PREPARATION AND REARRANGEMENT OF FUNCTIONALIZED 1-VINYLCYCLOPROPANOLS.
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The tetrahydropyranyl ether of 1-hydroxycyclopropanecarboxaldehyde, readily available from 1-hydroxycyclopropanecarboxylic acid, allows the preparation of functionalized 1-vinylcyclopropanols which undergo specific four- or five-membered ring annulations.
- Ollivier, J.,Salauen, J.
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Read Online
- Synthesis method 1- hydroxyl cyclopropane carboxylic acid and carboxylic ester (by machine translation)
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The reaction conditions of the 1 -hydroxycyclopropanecarboxylic acid, are mild and controllable :1 - in,hydroxycyclopropanecarboxylic acid 1 - reaction under the catalytic action of sodium nitrite and sulfuric acid, and the post-treatment is simple ;1 - through simple extraction and concentration to obtain,hydroxycyclopropanecarboxylic acid. 1 - The method. is suitable for industrial amplification and production of high-purity target products 1 - through simple extraction and concentration of,hydroxycyclopropanecarboxylic acid methyl ester as a raw material 60% - 70%. 2 through, a 1 -step reaction, and the method is simple in post-treatment; process conditions, through a simple extraction and concentration. (by machine translation)
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Paragraph 0034-0037; 0043-0045
(2020/03/17)
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- Synthesis and biological activities of potential metabolites of the non-nucleoside reverse transcriptase inhibitor efavirenz
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Studies on the biotransformation of the clinically important non-nucleoside reverse transcriptase inhibitor efavirenz have shown that oxidation and secondary conjugation are important components of the processing of this molecule in vivo. We have synthesized metabolites of efavirenz to confirm their structure and to evaluate their activity as antivirals.
- Markwalder, Jay A.,Christ, David D.,Mutlib, Abdul,Cordova, Beverly C.,Klabe, Ronald M.,Seitz, Steven P.
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p. 619 - 622
(2007/10/03)
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- 4,4-disubstitued-1,4-dihydro-2H-3,1-benzoxazin-2-ones useful as HIV reverse transcriptase inhibitors and intermediates and processes for making the same
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The present invention relates to benzoxazinones of formula I: STR1 or stereoisomeric forms or mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as an assay standard or reagent, and intermediates and processes for making the same.
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- BENZAMIDINE DERIVATIVES SUBSTITUTED BY CYCLIC AMINO ACID AND CYCLIC HYDROXY ACID DERIVATIVES AND THEIR USE AS ANTI-COAGULANTS
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This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.
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- N,N'-LINKED BIAZOLES. PART 5. SYNTHESIS OF PYRAZOLYL DIMERS BY THE REACTION OF 3-METHOXYCARBONYL-2-PYRAZOLINE WITH LEAD TETRAACETATE
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Contrary to a previous report by Akhrem et. al. (Tetrahedron Lett. 1973, 2655), the reaction of 3-methoxycarbonyl-2-pyrazoline with lead tetraacetate affords not only 3-methoxycarbonyl-1-(3-methoxycarbonyl-2-pyrazolin-1-yl)pyrazole (8) and 3-methoxycarbonyl-1-(1-methoxycarbonyl-1-cyclopropyl)pyrazole (9), but a complex mixture of pyrazoles and pyrazolines depending on the reaction conditions (LTA/pyrazoline ratio and temperature).The structures of all compounds have been established, and a new mechanism is proposed for the reaction.The oxidation of 8 with N-bromosuccinimide gave the symmetrical 3,3'-dimethoxycarbonyl-1,1'-bipyrazole (17).
- Mendoza, Javier de,Gonzales-Muniz, M. Rosario,Martin, M. Rosario,Elguero, Jose
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p. 2619 - 2628
(2007/10/02)
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- USE OF A β-TRIMETHYLSILYLETHOXYMETHYL ESTER AS A PROTECTING GROUP. A FACILE PREPARATION OF 1-HYDROXYCYCLOPROPANECARBOXYLIC ACID PHOSPHATE
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The potential use of β-trimethylsilylethoxymethyl (SEM) esters for temporary carboxyl blocking is illustrated in a preparation of the title compound.
- Logusch, E. W.
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p. 4195 - 4198
(2007/10/02)
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- CYCLOPENTENONES FROM 1,2-DISILOXYCYCLOBUTENE VIA SILYLATED 1-VINYLCYCLOPROPANOLS. APPLICATION TO THE SYNTHESIS OF DIHYDROJASMONE AND CIS-JASMONE
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An effective synthesis of 2,3-disubstituted 2-cyclopentenones involves C4 - C3 ring contraction of the readily available 1,2-disiloxycyclobutene followed by thermal C3 - C5 ring enlargement of trimethylsiloxyvinyl-cyclopropanes.To illustrate the convenience of this new approach the total syntheses of 2-methyl-3-p-tolyl-2-cyclopentenone, dihydrojasmone, and cis-jasmone are reported.
- Salauen, J.,Almirantis, Y.
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p. 2421 - 2428
(2007/10/02)
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