586966-54-3

Usage

Uses

tert-Butyl Pitavastatin is used to prepare hemicalcium salt.

InChI:InChI=1/C29H32FNO4/c1-29(2,3)35-26(34)17-22(33)16-21(32)14-15-24-27(18-10-12-20(30)13-11-18)23-6-4-5-7-25(23)31-28(24)19-8-9-19/h4-7,10-15,19,21-22,32-33H,8-9,16-17H2,1-3H3/b15-14+/t21-,22-/m1/s1

Upstream product

• 765-43-5 Cyclopropyl methyl ketone 
• 32249-35-7 methyl 3-cyclopropyl-3-oxopropanoate 
• 121660-11-5 2-cyclopropyl-4-(4-fluorophenyl)-3-(hydroxymethyl)quinoline 
• 154026-92-3 Tert-butyl (5S)-6-chloro-5-hydroxy-3-oxohexanoate 
• 540-88-5 acetic acid tert-butyl ester 
• 1234331-56-6 3-(chloromethyl)-2-cyclopropyl-4-(4-fluorophenyl)quinoline 
• 121660-37-5 2-cyclopropyl-4-(4-fluorophenyl)-3-formylquinoline 
• 154026-94-5 (4R-cis)-6-(chloromethyl)-2,2-dimethyl-1,3-dioxane-4-acetic acid,1,1-dimethylethyl ester 

Downstream Products

• 147526-32-7 pitavastatin calcium salt 
• 147526-32-7 pitavastatin 
• 574705-92-3 sodium (3R,5S,6E)-7-[2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl]-3,5-dihydroxyhept-6-enoate 
• 147511-70-4 (R)-1-phenylethanamine (3R,5S,E)-7-(2-cyclopropyl-4-(4-fluorophenyl)quinolin-3-yl)-3,5-dihydroxyhept-6-enoate 

Relevant academic research and scientific papers

Synthetic method of pitavastatin tert-butyl ester

The invention discloses a synthesis method of pitavastatin tert-butyl ester, which comprises the following steps: carrying out a reaction on (4R-Cis)-6-chloromethyl-2,2-dimethyl-1,3-dioxolane-4-tert-butyl acetate with a substance A under the action of a first base catalyst to obtain a substance B; oxidizing the substance B with an oxidizing agent to obtain a substance C; carrying out a reaction with 2-Cyclopropyl-4-(4-fluorophenyl)-quinoline-3-formaldehyde under the action of a second base catalyst to obtain a substance D; and finally, performing acid deprotection to obtain the pitavastatin tert-butyl ester. The method has the advantages of mild and controllable reaction conditions, wherein the reaction conditions of Julia olefination are free of requirement of ultralow-temperature reaction, so that the synthesis method has advantages of convenience and simplicity in operation, good stereoselectivity and high yield, and the synthesized pitavastatin tert-butyl ester is completely free of cis-isomer and high in purity.

For production of the precursor [...]

PROBLEM TO BE SOLVED: To provide a precursor compound of pitavastatin calcium excellent in safety and cost with high yield and high selectivity in a mild condition.SOLUTION: A method for producing a precursor compound of pitavastatin calcium of formula 1 is characterized by reacting a compound of formula 2 with a compound of formula 3 in the presence of an alkali metal salt selected from alkali metal carbonate, alkali metal acetate, and alkali metal propionate. (In the formulae, Ris a C-Calkyl group, and Ris an aryl group, an aralkyl group, or an alkyl group.)

Method for preparing statin raw material drug intermediate by use of improved Julia olefination as key step

The invention relates to a method for preparing a statin raw material drug intermediate by use of improved Julia olefination as a key step, and mainly solves the problems of high construction cost of a chiral center for preparing of the statin raw materia

3,5-dihydroxyhept-6-enoic acid derivative preparation method

The invention relates to a preparation method of 3, 5-dihydroxy-6-heptenoic acid derivatives. The preparation method comprises the steps of hydrolyzing crude statin ester to form a water-soluble alkali metal salt, extracting by using a solvent to remove impurities which cannot be dissolved into water, and converting at high yield to form ester with relatively high purity; then, purifying the ester by using a recrystallization way to obtain pure statin ester; and finally, converting the pure statin ester at high yield to form statin calcium, namely the 3, 5-dihydroxy-6-heptenoic acid derivatives. The 3, 5-dihydroxy-6-heptenoic acid derivatives, namely rosuvastatin calcium and pitavastatin calcium, synthesized by using the preparation method are high in purity and total yield, relatively low in cost and beneficial to mass production.

New statine intermediate, and using the same pitavastatin, rosuvastatin, and method of manufacturing cerivastatin [...]

The present invention provides a novel statin intermediate represented by chemical formula 1, and a method for producing pitavastatin, rosuvastatin, cerivastatin and fluvastatin by using the intermediate. (In chemical formula 1: n = 1, 2 or 3; Ar = a phenyl group or a phenyl group substituted with a C1-C4 alkyl or C6-C10 aryl, a naphthyl group or a naphthyl group substituted with a C1-C4 alkyl or C6-C10 aryl, or an anthracene group or an anthracene group substituted with a C1-C4 alkyl or C6-C10 aryl; and R1 is a C1-C8 alkyl, secondary alkyl, tertiary alkyl, aryl or aralkyl.)

NOVEL BORONATE ETHER INTERMEDIATES FOR PREPARATION OF STATIN COMPOUNDS, PREPARATION METHOD THEREOF AND PREPARATION METHOD OF STATIN COMPOUNDS USING SAID BORONATE ETHER INTERMEDIATES

The present invention relates to a novel boronate ether compound and a manufacturing method thereof. Provided is a novel boronate ether compound denoted by chemical formula 1 or chemical formula 2 as an intermediate to manufacture rosuvastatin calcium or pitavastatin calcium which is one of the statin based compounds to reduce the level of low density lipoprotein (LDL) of patients who have hyperlipidemia and are accordingly cured, and statin compounds with high purity are easily manufactured and separated compared with an existing patented method and are easily provided in a method of mass production.

AN IMPROVED PROCESS FOR THE PREPARATION OF CHIRAL DIOL SULFONES AND STATINS

The present invention relates to an improved process to prepare chiral diol sulfones of formula (I), wherein R1 and R2 each independently represent group selected from C1-4 alkyl, C1-4 alkenyl, C3-6 cycloalkyl, C6-10 aryl or C7-12 aralkyl, each of R1 and R2 may be substituted and wherein R1 and R2 may form a ring together with the C-atom; R3 represents group selected from C1-5 alkyl, aryl or aralkyl.

METHOD FOR PREPARING AN INTERMEDIATE OF PITAVASTATIN OR OF THE SALT THEREOF

The present invention relates to a method for preparing (4R,6S)-(E)-6-[2-(2-cyclopropyl)-4-(4-fluorophenyl)quinolin-3-yl)-vinyl-2,2-dimethyl-1,3-dioxan-4-yl]acetic acid ester derivative, which is an intermediate of pitavastatin or of the salt thereof, into a crystalline solid form. In addition, the present invention relates to a novel solvate of the intermediate, and to a method for preparing pitavastatin or the salt thereof using the intermediate.

NOVEL POLYMORPHS OF PITAVASTATIN CALCIUM

The present invention provides a solid of pitavastatin tert-butyl ester and process for its preparation. The present invention also provides a novel crystalline form of pitavastatin calcium, process for its preparation and pharmaceutical compositions comprising it.

Process for Preparing Pitavastatin, Intermediates and Pharmaceuctically Acceptable Salts Thereof

Processes for preparing pravastatin, intermediates and pharmaceutically acceptable salts thereof are provided Crystalline forms of pravastatin, intermediates and pharmaceutically acceptable salts thereof are also disclosed.