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 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 intermediates and methods for their preparation by Friedel-Crafts acylation.
摘要翻译:本发明涉及用于制备他汀类衍生物的合成方法,该方法通过式I的关键中间体进行,其中X是卤素,酰氧基,活化的烃氧基,活化的烃基硫基或N(CH 3) OCH 3,R a是羟基保护基,R b是羧基保护基,以及对于 式I化合物,其进一步的中间体及其通过Friedel-Crafts酰化制备的方法。
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:
A process for the preparation of compounds of formula (1), by enzymatic acylation to form compounds of formulae (3a) and (3a) and then reacting the compound of formula (3a) with a compound introducing the radical of formula —CH2—COOR8, R8 being an organic radical, and then reducing, and optionally hydrolysing, the resulting compound of formula (4).
摘要:
A process for the preparation of an 1,1-disubstituted oxirane is disclosed, wherein an organic sulphide is reacted in a polar solvent with an educt containing a leaving group attached to a primary or secondary carbon atom, and/or the sulfonium salt formed in this way is reacted with a ketone in presence of a base and a polar solvent. Oxiranes of the type obtained may be further converted into the corresponding α-hydroxyketone or α-aminoketone, either in one step by subjecting to aerobic oxidation in the presence of a transition metal catalyst, or in two steps by hydrolyzation in the presence of an aqueous acid to the corresponding dialcohol and subsequent selective oxidation. Further described are some novel epoxide intermediates. The α-hydroxyketones and α-aminoketones thus obtainable are useful inter alia as photoinitiators.
摘要:
The present invention relates to the use of metal complex compounds having hydrazide ligands as oxidation catalysts. Further aspects of the invention are formulations comprising such metal complex compounds, novel metal complex compounds and novel ligands. The metal complex compounds are used especially for enhancing the action of peroxides, for example in the treatment of textile material, without at the same time causing any appreciable damage to fibers and dyeings. There is also no appreciable damage to fibers and dyeings if these metal complexes are used in combination with an enzyme or a mixture of enzymes.
摘要:
A process for the preparation of an 1,1-disubstituted oxirane is disclosed, wherein an organic sulphide is reacted in a polar solvent with an educt containing a leaving group attached to a primary or secondary carbon atom, and/or the sulfonium salt formed in this way is reacted with a ketone in presence of a base and a polar solvent. Oxiranes of the type obtained may be further converted into the corresponding α-hydroxyketone or α-aminoketone, either in one step by subjecting to aerobic oxidation in the presence of a transition metal catalyst, or in two steps by hydrolyzation in the presence of an aqueous acid to the corresponding dialcohol and subsequent selective oxidation. Further described are some novel epoxide intermediates. The α-hydroxyketones and α-aminoketones thus obtainable are useful inter alga as photoinitiators.
摘要:
The invention relates to novel ligands of the phosphanylbenzothiophenyl-dihydroisoxazoline, phosphanyl-dihydrooxazolyl-indole and phosphanyl-dihydrooxazolyl-benzofuran type, especially compounds of formula I and mixtures of such compounds, wherein X is oxygen, sulfur, selenium or NQ, wherein Q is unsubstituted or substituted aryl, or alkyl or substituted alkyl; n is 0, 1, 2, 3 or 4; A1 and A2 are each an organic radical capable of bonding to phosphorus, especially unsubstituted or substituted alkyl, unsubstituted or substituted aryl, unsubstituted or substituted heterocyclyl, unsubstituted or substituted cycloalkyl, or —N(D)2 wherein D2 is alkyl or substituted alkyl; or A1 and A2 together with the bonding phosphorus atom form a ring, which may be unsubstituted or substituted; Y, Y′, Y″ and Y′″ are each independently of the other hydrogen or alkyl, substituted alkyl, unsubstituted or substituted aryl, or unsubstituted or substituted heterocyclyl, at least one of the radicals Y, Y′, Y″ or Y′″ being one of the mentioned radicals with the exception of hydrogen; and Z, when present, is a substituent, it being possible when a plurality of substituents Z is present for those substituents to be selected independently of one another, and to processes for their preparation, to novel precursors and intermediates, to complexes with the said ligands, to their preparation and to their use as catalysts in organic synthesis (especially asymmetric organic synthesis).