- Silica gel-mediated rearrangement of allylic acetates. Application to the synthesis of 1,3-enynes
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Silica gel was found to efficiently promote the rearrangement of allylic acetates into their most stable regioisomers under microwave irradiation. The reaction is easy to perform and eco-friendly. This method was applied to the metal-free synthesis of 1,3-enynes.
- Serra-Muns, Anna,Guerinot, Amandine,Reymond, Sebastien,Cossy, Janine
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supporting information; experimental part
p. 4178 - 4180
(2010/08/07)
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- PROCESS FOR PREPARING TERBINAFINE
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A process for preparing terbinafine or a salt thereof having high purity.
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Page/Page column 15
(2010/11/27)
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- IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE HYDROCHLORIDE AND NOVEL CRYSTALLINE FORM OF TERBINAFINE
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Improved process for the preparation of Terbinafme Hydrochloride compound of formula (I): substantially free of Genotoxic impurity compound of formula (II) and Novel crystalline form of Terbinafine.
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Page/Page column 20
(2010/11/28)
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- Process for the preparation of terbinafine and salts thereof
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A process for the preparation of Terbinafine and salts thereof by reacting 1-chloro-6,6-dimethylhept-2-en-4-yne and N-methyl-N-(1-naphthylmethyl)amine in a basic aqueous medium is disclosed. Also disclosed is a process for the preparation of 1-chloro-6,6-dimethylhept-2-en-4-yne.
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Page/Page column 10
(2008/06/13)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF TERBINAFINE HYDROCHLORIDE
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The present invention relates to an improved process for preparation of terbinafine hydrochloride ,which is (E) - N- Methyl -N-(1-Naphtylmethyl)-6,6-dimethylhept-2-ene-4-ynyl-1-amine has the formula (I), which comprises reacting t-butylacetylene with ethylmagnesium bromide in THF (ii) adding acrolein at a temperature in the range of 0-10o C to get , 6,6-dimethyl-hept-1-ene-4-yne-3-ol, (iii) reacting it with a mixture of phosphorous oxychloride and hydrochloric acid in methanol (iv) extracting the reaction mass with aliphatic/aromatic solvent and removing the solvent (v) reacting the residue with N-(1-naphtylmethyl)methyl amine in the presence of a base to give Terbinafine (vi) adding hydrochloric acid and extracting the Terbinafine Hcl formed with a chlorinated solvent and (vii) recovering the chlorinated solvent under vacuum and adding ethylacetate to separate Terninafine hydrochloride which is filtered and dried.
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Page/Page column 9-10
(2010/02/14)
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- A process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol
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The invention provides a process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between -40°C to +20°C, quenching the reaction mixture and isolating the product.
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- Process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol
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The invention provides a process for the preparation of 6,6-dimethylhept-1-en-4-yn-3-ol comprising of reacting t-butylacetylene with a proton-extracting agent selected from the group consisting of an organometallic compound and metallic lithium to form a t-butylacetylide, reacting the acetylide with acrolein at temperatures between ?40° C. to +20° C., quenching the reaction mixture and isolating the product.
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- Pyrazole compounds, insecticidal and acaricidal compositions and use
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There are disclosed a pyrazole compound represented by the formula, STR1 wherein the substituents of R1 to R8 and the symbol Z have the specified meanings as described in the text, an insecticidal and acaricidal composition containing the same, use of said composition for control of insects and mites and a method of preparing said compound, and its intermediate.
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- Intermediate compounds for an insecticidal and acaricidal pyrazole compound
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There are disclosed intermediate compounds of the formula, STR1 wherein the substitutents of R1 to R7 and R9 have the same meanings as described in the text, for producing a insecticidal and acaricidal pyrazole compound represented by the formula, STR2 wherein the substituents of R1 ' to R8 and the symbol Z have the specified meanings as described in the text.
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- Synthesis and Antifungal Activity of (E)-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthalenemethanamine (SF 86-327) and Related Allylamine Derivatives with Enhanced Oral Activity
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The allylamine derivatives are a new class of synthetic antifungal agents inhibiting fungal squalene epoxidase.A new subclass, which features an acetylene group conjugated with the allylamine double bond, is characterized by enhanced antifungal activity, especially on oral treatment of guinea pig dermatophytoses.Increased branching of the alkyl group next to the triple bond led to the tert-butylacetylene derivative SF 86-327, a compound with strikingly increased activity in vitro and in vivo, which is now under clinical evaluation.Versatile synthetic routes, comparative biological data, and structure-activity relationship are presented.
- Stuetz, Anton,Petranyi, Gabor
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p. 1539 - 1543
(2007/10/02)
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