113240-61-2Relevant academic research and scientific papers
Novel boronate esters
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Page/Page column 11, (2008/06/13)
The present invention relates to optically active boronate derivatives which are useful as intermediates for the synthesis of HMG-CoA enzyme inhibitors such as atorvastatin, cerivastatin, rosuvastatin, pitavastatin, and fluvastatin.
Process for the production of 3,5,6-trihydroxyhexanoic acid derivative
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, (2008/06/13)
A compound of a 3,5,6-trihydroxyhexanoic acid derivative of the formula: STR1 wherein P1 and P2 are independently hydrogen atoms or hydroxy-protecting groups, or together form a ring, and R is an alkyl group is effectively prepared by a process comprising steps of: reacting a butyronitrile derivative of the formula: STR2 wherein P1 and P2 are the same as defined above with an α-haloacetate of the formula: wherein X is a halogen atom, and R is the same as defined above in the presence of a metallic catalyst selected from the group consisting zinc and zinc-copper to form a keto acid derivative of the formula: STR3 wherein P1, P2 and R are the same as defined above, and then reducing the obtained keto-acid derivative of the formula (IV).
Pyrimidinyl-substituted hydroxyacids, lactones and esters and pharmaceutical compositions containing them
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, (2008/06/13)
Compounds of formula I wherein R1, R2, Q, X and Y have various significances,in free acid form, or in the form of an ester or δ-lactone thereof, or in salt form as appropriate, are described. They are indicated for use as hypolipoproteinemic and anti-athe
A Highly Stereoselective Route to the Four Stereoisomers of a Six-Carbon Synthon
Prasad, Kapa,Chen, Kau-Ming,Repic, Oljan,Hardtmann, Goetz E.
, p. 307 - 310 (2007/10/02)
The syntheses of chiral synthones 13-16 are described utilizing the chiral pool approach starting from either S- or R-malic acid.
Processes for the synthesis of diprotected R[R*,S*]-3,5-dihydroxy-6-oxohexanoate esters
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, (2008/06/13)
Process for the synthesis of compounds of the formula STR1 in R[R*,S*] enantiomeric form, wherein each P1 is independently an hydroxy group-protecting group, and R2z is C1-4 alkyl, benzyl or allyl, comprising, as a key step when R2z is R2x, the reaction of the compound of the formula STR2 in (S) enantiomeric form with a compound of the formula to obtain a compound of the formula STR3 in (S) enantiomeric form, and, as a key step when R2z is R2y, the reaction of a compound of the formula STR4 in (S) enantioimeric form with a compound of the formula to obtain a compound of the formula STR5 in (S) enantiomeric form, wherein R2x is primary or secondary C1-4 alkyl, benzyl or allyl, R2y is C1-4 alkyl not containing an asymmetric carbon atom, and R3 ' is methyl or ethyl, processes for the synthesis of compounds of the formula STR6 comprising reacting a compound of the formula STR7 with the reaction product of a strong base and a compound of the formula STR8 optionally followed by, when R2z is allyl, cleavage of the allyl and P1 groups to obtain the corresponding compound of the formula STR9 wherein each R7 is methyl or ethyl, R is as defined in the specification, and each P1 independently and R2z are as defined above, and the compounds of the formula STR10 wherein R and each R7 are as defined above.
Imidazole analogs of mevalonolactone and derivatives thereof for use in inhibiting cholesterol biosynthesis and lowering blood cholesterol level
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, (2008/06/13)
Compounds of the formula STR1 and the pharmaceutically acceptable acid addition salts thereof, wherein the various substituents are defined hereinbelow and the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.
Pyrazolopyridine analogs of mevalonolactone and derivatives thereof useful for inhibiting cholesterol biosynthesis in mammals
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, (2008/06/13)
Compounds of the formula STR1 and processes for and intermediates in the synthesis thereof, pharmaceutical compositions comprising such a compound and the use of such compounds for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis.
