摘要:
The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要:
Synthesis methods for the preparation of intermediates which are suitable for the preparation of statin derivatives, and especially to synthesis methods for the intermediate of formula (VI) wherein Ra′ and Rc′ are each independently of the other hydrogen or hydroxy-protecting group, or together are a bridging hydroxy-protecting group; and Rb is a carboxy-protecting group.
摘要:
The invention relates to a process for the preparation of (bis)acylphosphanes of formula I, wherein n and m are each independently of the other 1 or 2; R1 if n=1, is e.g. unsubstituted or substituted C1-C18alkyl or C2-C18alkenyl, or phenyl, R1 if n=2, is e.g. a divalent radical of the monovalent radical defined above; R2 is e.g. C1-C18alkyl, C3-C12cycloalkyl, C2-C18alkenyl, mesityl, phenyl, naphthyl; R3 is one of the radicals defined under R1; the process comprises the steps a) contacting e.g. elemental phosphorous [P]∞, P(Hal)3 with a reducing metal optionally in the presence of a catalyst or an activator in a solvent to obtain metal phosphides Me3P or Me′3P2, wherein Me is an alkali metal and Me′ is an earth alkali metal or to obtain metal polyphosphides b) optionally adding a proton source, optionally in the presence of a catalyst or an activator to obtain metal dihydrogen phosphides MePH2; c) subsequent acylation reaction with m acid halides of formula III or m carboxylic acid esters of formula IV or, in case that in formula I m=1, with one carboxylic ester of formula IV followed by one acid halide of formula III or vice versa, wherein R is the residue of an alcohol and R2 is as defined above; d) alkylation reaction subsequent reaction with an electrophilic agent R1Hal or other electrophilic agents to obtain the compounds of formula I. An oxidation step may follow to obtain mono- and bisacylphosphane oxides or mono- and bisacylphosphane sulfides, which are used as photoinitiators.
摘要:
The present invention relates to novel processes for the preparation of optically active 3-aminocarboxylic acids and their esters, in particular processes for the preparation of optically active compounds of the formula IA or IB as free bases or as acid addition salts thereof, in which the radicals are as defined in the description; in particular using the catalytic hydrogenation of olefinic precursors in the presence of platinum on alumina as a catalyst and the removal of chiral auxiliary groups from salt precursors; and novel process sections in the route for their synthesis, and processes for the preparation of biologically, in particular pharmacologically, active compounds, which comprise the novel processes.
摘要:
The invention relates to novel synthesis methods for the preparation of the intermediates, which are suitable for the preparation of statin derivatives, especially to novel synthesis methods of the intermediate of formula VI wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group or together are a bridging hydroxy-protecting group, and Rb is a carboxy-protecting group, which methods are carried out by conversion of the intermediate of formula XIX wherein Ra and Rc are each independently of the other hydrogen or a hydroxy-protecting group, and Rb is a carboxy-protective group.
摘要:
The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要:
The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要:
The invention relates to novel synthesis methods for the preparation of statin derivatives, which methods proceed by way of a key intermediate of formula I wherein X is halogen, acyloxy, activated hydrocarbyloxy, activated hydrocarbylthio or —N(CH3)OCH3, Ra is a hydroxy-protecting group and Rb is a carboxy-protecting group, and, as well as to the compound of formula I, to further new intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要:
The present invention relates to a new, selective process for the preparation of mono- and bisacylphosphanes of formula (I) n and m are each independently of the other 1 or 2; R1, if n=1, is e.g. phenyl R1, if n=2, is e.g. C1-C18alkylene or phenylene; R2 is e.g. C1-C18alkyl, phenyl or substituted phenyl; R3 is e.g. C1-C18alkyl, by (I) reacting a phosphorous halide of formula IIa or a phosphorous halide oxide of formula (IIb) or a phosphorous halide sulfide of formula (IIc) with an alkali metal in a solvent in the presence of a proton source; (2) subsequent reaction with m acid halides of formula (III) An oxidation step may follow to obtain mono- and bisacylphosphane oxides or mono-and bisacylphosphane sulfides.
摘要翻译:本发明涉及制备式(I)的单 - 和双酰基磷烷的新的选择性方法,n和m各自独立地为1或2; 如果n = 1,则为R 1。 苯基R 1,如果n = 2,则为例如。 C 1 -C 18亚烷基或亚苯基; R 2是例如。 C 1 -C 18烷基,苯基或取代的苯基; R 3是例如。 通过(I)使式IIa的卤化磷或式(IIb)的卤化磷氧化物或式(IIb)的卤化磷化物或式(Ⅳ) IIc)与碱金属在溶剂中在质子源存在下反应; (2)随后与式(III)的酰卤反应可以进行氧化步骤以获得单酰基和双酰基氧化膦或单酰基和双酰基磷烷硫化物。
摘要:
Disclosed is a composition comprising a charged particle of volume 5 nm3 to 50 million nm3 preferably having an inorganic core of SiO2, AI2O3, and/or TiO2, or a core essentially consisting of an organic pigment and/or pigment derivative, and a counter ion which is separable from the particle and is not covalently linked to the particle, said counter ion comprising a silicon atom which is directly bound to a carbon atom. Preferably, said charged particle comprises a dye attached to said inorganic core and said counter ion comprises a (poly)siloxane moiety linked via suitable bridge members to a quaternary, positively charged, nitrogen or phosphorus atom, or to a moiety carrying an anionic functional group. Said composition may be used e.g. in the form of a homogenous dispersion in an electrophoretic display.