1190399-91-7

Upstream product

• 1032903-63-1 4-(4-amino-5-isopropoxy-2-methylphenyl)-piperidine-1-carboxylic acid tert-butyl ester 
• 64695-96-1 1-bromo-5-fluoro-2-methyl-4-nitrobenzene 
• 1422-53-3 2-bromo-4-fluorotoluene 
• 1032903-62-0 4-[2-methyl-4-nitro-5-(propan-2-yloxy)phenyl]pyridine 
• 1035230-24-0 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-((2-isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1032903-52-8 4-(2-methyl-4-nitro-5-isopropoxyphenyl)-5,6-dihydropyridine-1(2H)-carboxylic acid tert-butyl ester 
• 375853-82-0 tert-Butyl 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-3,6-dihydro-1(2H)-pyridinecarboxylate 
• 1032903-50-6 1-chloro-2-methyl-4-nitro-5-(propan-2-yloxy)benzene 

Downstream Products

• 1380575-43-8 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine hydrochloride 
• 1032903-63-1 4-(4-amino-5-isopropoxy-2-methylphenyl)-piperidine-1-carboxylic acid tert-butyl ester 

Relevant academic research and scientific papers

CHEMICAL PROCESS FOR PREPARING PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF

PROBLEM TO BE SOLVED: To provide a process for preparing ceritinib and/or intermediates thereof. SOLUTION: There is provided a process for preparing (C2-1), an intermediate of ceritinib synthesis, comprising the step of reacting (A) with (B) in a solvent in the presence of at least one catalyst, wherein P is a protecting group and T and X1 independently denote Cl and the like. SELECTED DRAWING: None COPYRIGHT: (C)2021,JPOandINPIT

Chemical Process for Preparing Pyrimidine Derivatives and Intermediates Thereof

The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.

CHEMICAL PROCESS FOR PREPARING PYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF

PROBLEM TO BE SOLVED: To provide a method for producing intermediates for preparing ceritinib. SOLUTION: There is provided a method for preparing (C2-1), comprising reacting (A) with (B) in a solvent in the presence of at least one catalyst, wherein P is a protecting group and T and X1 can be independently C1 and the like. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT

Preparation method and application of ceritinib intermediate

The invention relates to a preparation method and application of a ceritinib intermediate, in particular to a preparation process of an intermediate which is 2,5-dichloro-N-(2-(isopropylsulfonyl) phenyl)pyrimidine-4-amine, and belongs to the field of medicine synthesis. The preparation method includes the detailed following steps that a compound 1-a, a compound 1-b, palladium acetate, 9,9-dimethyl-4,5-bis(diphenylphosphino)xanthene and alkali are added into a solvent, a reaction is conducted, and then the ceritinib intermediate can be prepared. The route is simple and short, operation is easy,production costs are lowered, and the preparation method is suitable for large-scale industrialized production.

Chemical Process for Preparing Pyrimidine Derivatives and Intermediates Thereof

The present disclosure relates to a method of synthesizing 5-chloro-N2-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N4-[2-(propane-2-sulfonyl)-phenyl]-pyrimidine-2,4-diamine (ceritinib) and/or intermediates thereof, their use as pharmaceuticals and pharmaceutical compositions and the use of intermediates for preparing ceritinib.

HYDRATE OF 2-ISOPROPOXY-5-METHYL-4-(PIPERIDIN-4-YL) ANILINE DIHYDROCHLORIDE, PREPARATION METHOD AND USE OF THE SAME

The present invention relates to 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate and a preparation method of the same. The 2-isopropoxy-5-methyl-4-(piperidin-4-yl) aniline dihydrochloride monohydrate has a very good crystal form and is well suitable for recrystallization purification; further, the effect of impurity removal effect is very good, and any single impurity can be controlled less than 0.1%.

A MODIFIED PROCESS FOR THE PREPARATION OF CERITINIB AND AMORPHOUS FORM OF CERITINIB

The present invention is related to an improved process for the preparation of ceritinib with high yield and high purity. The present process is cost effective and feasible in large scale production also. The present invention also related to a stable amorphous form of ceritinib and its preparation. The present invention also relates to a process for the preparation of Crystalline form A of Ceritinib.

Preparation method of 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride

The invention relates to a preparation method of 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride. The preparation method comprises the following steps: carrying out a nucleophilic substitution reaction, a coupling reaction and a reduction reaction by taking 1-chloro-5-fluoro-2-methyl-4-nitrobenzene as a starting material so as to obtain 1-benzyl-4-(5-isopropoxy-2-methyl-4-nitrophenyl)-1,2,3,6-tetrahydropyridine; carrying out a reduction reaction on the 1-benzyl-4-(5-isopropoxy-2-methyl-4-nitrophenyl)-1,2,3,6-tetrahydropyridine again to obtain the 2-isopropoxy-5-methyl-4-(piperidine-4-yl) aniline dihydrochloride. The method does not use catalysts such as platinum and rhodium, is simple and convenient in reaction technology and high in yield, avoids the high pressure reaction condition of the existing process, improves the safety, and shortens the reaction time, thus being suitable for mass production.

Preparation color Switzerland for Nepal new intermediate and its preparation method

The invention relates to intermediates, namely a compound 1 of a formula (1) as shown in the specification and a compound 2 of a formula (2) as shown in the specification, for preparing ceritinib, or a chemically acceptable salt of the compound 2, wherein R represents the benzylic group of saturated or unsaturated aromatic ring methylene or heteroaromatic ring methylene, and X represents a halogen. The invention relates to a method for preparing a compound 4 by use of the new intermediates, namely the compound 1 and the compound 2, wherein the step of reduction from the compound 1 to the compound 2 is performed by use of a hydroboron or a composition thereof and an alcohol solvent; the compound 2 is reduced by use of a catalytic hydrogenation or transfer hydrogenation method to generate the compound 4. The route of preparing the compound 4 by use of the compound 1 and the compound 2 has the advantages that the chemical reduction step is combined with a catalytic hydrogenation, the use of expensive platinum dioxide is avoided and the cost of synthesizing the intermediate 4 of the ceritinib is effectively reduced.

Preparation method for ceritinib and intermediate thereof

The invention provides a preparation method for ceritinib and an intermediate thereof. The method comprises the following steps: (1) coupling the compound 1-dihydrochloride with the compound 2,5-dichloro-N-(2-(isopropylsulfonyl)phenyl)pyrimidin-4-amine (a compound 3) so as to produce 5-chloro-N2-(2-isopropanolato-5-methyl-4-(piperid-4-yl)phenyl)-N4-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine dihydrochloride (a compound 4, i.e., ceritinib dihydrochloride); and (2) subjecting the compound 4 to dissociation so as to produce ceritinib. The preparation method provided by the invention is low in cost and high in yield, and the purity of the intermediate in each step is 99.5% or above, so high purity of ceritinib is guaranteed. The method is few in steps, simple to operate and suitable for industrial production and has great application value.