摘要:
A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.
摘要:
A process for the preparation of L-ribavirin on an industrial scale is described which comprises the reaction of glycosylation of 3-substituted triazoles in the presence of a Lewis acid. Said process comprises: a) the reaction of a triazole of the formula with a protected ribofuranose of the formula (II) b) the removal of the Pg groups and, optionally, the conversion into a carboxyamide group of the R2 group of the compound obtained of the formula (III)
摘要:
A process for preparing 2′,3′-didehydro-2′,3′-dideoxynucleosides and 2′,3′-dideoxynucleosides is described, which comprises the reductive elimination reaction of a compound of formula in which X, Y, P′ is H or a protecting group and B is a natural or modified, optionally substituted purine or pyrimidine base or a five- or six-membered monocyclic or eleven- or twelve-membered bicyclic, optionally substituted heterocyclic system containing at least one nitrogen atom, by reaction with zinc metal and a suitable activating agent, characterized in that the divalent zinc is removed by precipitation, from an organic phase, of the corresponding zinc sulfide, by adding a solution of a mineral sulfide to the organic phase.
摘要:
The present invention relates to a process for preparing 2,5-disubstituted 3-alkyl-thiophenes and more particularly to a process for preparing them that comprises an acylation reaction in position 5 of 2-substituted 3-alkylthiophenes. This process does not need reagents which are difficult to handle and does not need anhydrous conditions or inert atmosphere. The resulting product is obtained in high purity.
摘要:
The present invention relates to a process for preparing 5′-acetylstavudine, an intermediate which is useful in the preparation of 2′,3′-didehydro-3′-deoxythymidine, an active principle with antiviral action which is commonly known as stavudine (D4T).
摘要:
A description is given here of a novel process for the synthesis of N-carboxyanhydride of formula VI by reacting (3S)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid with triphosgene in dioxane; a description is also given of a process for the synthesis of (S)-N-tert-butyl-1,2,3,4-tetrahydroisoquinoline-3-carboxyamide by treating the N-carboxyanhydride VI so obtained with tert-butylamine.
摘要:
A takeup drum, particularly for wire drawing machines, having a fluid cooling unit, the drum comprising: a cylindrical body, which is rotatable about a central axis and is supported, through bearings, by the fixed frame of the machine; a chamber that is formed in the body; and a drum cooling unit that is arranged in the chamber. The cooling unit comprises: at least one circular sector that is located proximate to the internal lateral surface of the body and is connected to the fixed frame that supports the cylindrical drum body; and at least one nozzle for introducing the cooling fluid, located proximate to the outer surface of the sector, so as to form a jacket of cooling fluid that flows over the internal lateral surface of the body.
摘要:
17-Heterocyclyl-5.alpha.-14.beta.-androstane, androstene and androstadiene of formula (I): ##STR1## wherein: Y is oxygen or guanidinoimino, when a double bond exists at position 3;Y is hydroxy, OR.sup.2 or SR.sup.2, when a single bond exists at position 3;R is a saturated or unsaturated mono- or biheterocyclic ring, containing one or more heteroatoms selected from the group consisting of oxygen, sulfur, and nitrogen, unsubstituted or substituted by one or more of halogen, hydroxymethyl, alkoxy, amino, alkylamino, dialkylamino, cyano, nitro, sulfonamido, C.sub.1 -C.sub.6 lower alkyl or COR.sup.3 ; andR.sup.1 is hydrogen, methyl, ethyl or n-propyl substituted by OH or NR.sup.4 R.sup.5.
摘要:
The present invention relates to new cyclopentanperhydrophenanthren-17-(hydroxy or alkoxy)-17-(aryl or heterocyclyl)-3.beta.-derivatives, active on the cardiovascular system, to a process for their preparation and to pharmaceutical compositions containing them. The invention relates to compounds of general formula (I) ##STR1## wherein X is O or S and R, R.sup.1 and R.sup.2 is selected from various groups.
摘要:
A process for the selective oxidation of a primary or secondary alcohol to an aldehyde or ketone and for the oxidation of a 1,2-diol to an .alpha.-ketol or .alpha.-diketone, which comprises contacting the alcohol or 1,2-diol with o-iodoxybenzoic acid. This process is suited for selective oxidation of alcohols containing easily oxidizable groups, such as amino or thioether groups and easily oxidizable heterocycles.