1032903-63-1

Usage

Uses

Used in Pharmaceutical Research:
Tert-butyl 4-(4-amino-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate is used as a chemical intermediate for the synthesis of novel bioactive compounds with potential therapeutic properties. Its unique structural features make it a promising candidate for the development of new drugs.
Used in Drug Development:
In the pharmaceutical industry, tert-butyl 4-(4-amino-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylate is used as a building block for the creation of new drug molecules. Its potential pharmacological activities and structural characteristics make it a valuable asset in the search for innovative treatments and therapies.

Upstream product

• 60710-39-6 3-bromo-p-cresol 
• 1254062-68-4 2-bromo-4-isopropoxy-1-methylbenzene 
• 1202858-68-1 1-bromo-5-isopropoxy-2-methyl-4-nitrobenzene 
• 24424-99-5 di-tert-butyl dicarbonate 
• 1190399-91-7 2-isopropoxy-5-methyl-4-(4-piperidinyl)aniline hydrochloride 
• 64695-96-1 1-bromo-5-fluoro-2-methyl-4-nitrobenzene 
• 1032903-62-0 4-[2-methyl-4-nitro-5-(propan-2-yloxy)phenyl]pyridine 
• 1692-15-5 4-pyridylboronic acid 
• 1032903-52-8 4-(2-methyl-4-nitro-5-isopropoxyphenyl)-5,6-dihydropyridine-1(2H)-carboxylic acid tert-butyl ester 
• 1035230-24-0 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-((2-isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 452-73-3 2-chloro-4-fluorotoluene 
• 1032903-50-6 1-chloro-2-methyl-4-nitro-5-(propan-2-yloxy)benzene 
• 112108-73-3 1-chloro-5-fluoro-2-methyl-4-nitrobenzene 
• 807618-13-9 (1-(tert-butoxycarbonyl)piperidine-4-yl)zinc(II) iodide 

Downstream Products

• 1032903-64-2 4-(4-{5-chloro-4-[2-(propane-2-sulfonyl)phenylamino]pyrimidin-2-ylamino}-5-isopropoxy-2-methylphenyl)piperidine-1-carboxylic acid tert-butyl ester 
• 1380575-43-8 5-chloro-N²-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N⁴-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine hydrochloride 
• 1445894-96-1 N₂-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)-5-methylpyrimidine-2,4-diamine 
• 1445895-03-3 5-chloro-N₂-(2-isopropoxy-5-methyl-4-(1-ethylpiperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1445895-04-4 5-chloro-N₂-(2-isopropoxy-5-methyl-4-(1-isopropylpiperidin-4-yl)phenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1445895-08-8 5-chloro-N₂-(4-(1-(2,2-difluoroethyl)piperidin-4-yl)-2-isopropoxy-5-methylphenyl)-N₄-(2-(isopropylsulfonyl)phenyl)pyrimidine-2,4-diamine 
• 1190399-47-3 1-(4-(4-((5-chloro-4-((2-(isopropylsulfonyl)phenyl)amino)pyrimidin-2-yl)amino)-5-isopropoxy-2-methylphenyl)piperidin-1-yl)-2-(dimethylamino)ethanone 
• 1445895-25-9 2-(4-(5-isopropoxy-4-((4-((2-(isopropylsulfonyl)phenyl)amino)-5-methylpyrimidin-2-yl)amino)-2-methylphenyl)piperidin-1-yl)ethanol 
• 1445895-27-1 N₂-(2-isopropoxy-4-(1-(2-methoxyethyl)piperidin-4-yl)-5-methylphenyl)-N₄-(2-(isopropylsulfonyl)phenyl)-5-methylpyrimidine-2,4-diamine 
• 1190399-91-7 5-chloro-N²-[2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl]-N⁴-[2-(isopropylsulfonyl)phenyl]pyrimidine-2,4-diamine dihydrochloride 
• 1380575-43-8 5-chloro-N₂-(2-isopropoxy-5-methyl-4-(piperidin-4-yl)phenyl)-N₄-(2-(propane-2-sulfonyl)phenyl)pyrimidine-2,4-diamine dihydrochloride 

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.

Anti-tumor compound and application thereof

The present invention relates to a compound having a structure of formula I, in which the substituent R is C6-C8 cycloalkyl, aryl, n R1 substituted aryl, or n R1 substituted C6-C8 cycloalkyl, n being1-4; wherein the R1 is independently selected from a halogen atom, a C1-C6 alkyl group, a C2-C4 alkenyl group, a C2-C3 alkynyl group, a fluorine-substituted C1-C4 alkyl group, a phenyl group, a substituted phenyl group, a nitro group, a pyridyl group, a pyrrolyl group, a pyrazinyl group, a piperazinyl group and a furyl group; the R2 is a C1-C3 alkyl group; R3 is a C1-C4 alkyl group; and R4 is a compound containing o-aminophenyl, m-aminophenyl, p-aminophenyl, pyrrolyl, pyridyl, piperidyl, piperazinyl, pyrazinyl, pyrimidinyl and quinolyl.

Ceritinib intermediate and method for preparing ceritinib

The invention relates to a ceritinib intermediate and a method for preparing ceritinib. A ceritinib intermediate compound is 4-isopropoxy-5-guanidyl-2-N-substituted piperidine-4-base toluene nitrate (VII). The method includes carrying out substation reaction on 2-nitro-4,5-dimethyl chlorobenzene and isopropyl alcohol in the presence of alkali to generate compounds III; carrying out condensation onthe compounds III and halogenated acetaldehyde di-acetal and carrying out reduction ring formation by ammonia-ammonium chloride-sodium borohydride to obtain compounds IV; carrying out amino protection to obtain compounds V; carrying out catalytic hydrogenation in solvents and carrying out nitro reduction to obtain amino so as to obtain compounds VI; carrying out reaction on the compounds VI and cyanamide to obtain compounds VII. The ceritinib can be prepared from the compounds VII by the aid of the method. The ceritinib intermediate and the method have the advantages of inexpensive and easilyavailable raw materials, simplicity and convenience in operation, high elementary reaction selectivity, low wastewater quantity and green environmental protection.

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

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.

CONDENSED-RING PYRIMIDYLAMINO DERIVATIVE, PREPARATION METHOD THEREFOR, AND INTERMEDIATE, PHARMACEUTICAL COMPOSITION AND APPLICATIONS THEREOF

Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b' to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.

Anaplastic lymphoma kinase (ALK) inhibitor, and preparation method and application thereof

The invention relates to a compound as shown in a formula (I) which is described in the specification, and a pharmaceutical composition and a preparation method thereof. The compound can be used as anALK inhibitor for treatment of diseases mediated by ALK. The invention further relates to application of the compound as shown in the formula (I) and the pharmaceutical composition thereof to preparation of drugs used for treating diseases mediated by ALK.

Boryl-substituted aniline-based protein kinase inhibitor

The present invention discloses a compound capable of regulating protein kinase activity and used for treating or preventing protein kinase-related diseases, particularly relates to a boryl-substituted aniline-based protein kinase inhibitor, belongs to the compound capable of regulating the activity of anaplastic lymphoma kinase (ALK), and provides a preparation method of the compounds, and pharmaceutical uses of the compounds in treatment or prevention of ALK-related diseases.

A method for preparing color Switzerland for Nepal

The invention discloses a method for preparing ceritinib, belonging to the field of chemical pharmacy. The method comprises the following steps: by taking 3-bromine-4-methylphenol as an initial raw material, performing phenolic hydroxyl isopropylation, nitration, coupling and reduction reaction, obtaining a midbody 1, by further taking o-nitro fluorobenzene as another initial raw material, performing isosulfhydrylation, oxidation, reduction and pyrimidine, obtaining a midbody 2, performing coupling reduction on the midbody 1 and the midbody 1, obtaining ceritinib which is protected by BOC acid anhydride, and finally removing a t-butyloxycarboryl protecting group, and obtaining ceritinib. The method is simple and feasible to operate, relatively high in yield, small in pollution and applicable to industrial production.