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Upstream product

• 3943-89-3 Ethyl protocatechuate 
• 19249-03-7 triethylene glycol di-(p-toluenesulfonate) 

Downstream Products

• 610798-31-7 N-(3-ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine 

Relevant academic research and scientific papers

Synthesis and radical polymerisation of methacrylic monomers with crown ethers or their dipodal counterparts in the pendant structure

The synthesis and radical polymerisation of methacrylic monomers with benzo-12-crown-4, benzo-15-crown-5, benzo-18-crown-6, and their dipodal counterparts in the ester residue is described. The radical polymerisation of the monomers in solution was carried out at different temperatures, and the polymerisation kinetics curves were obtained by direct measurement of the instantaneous monomer concentrations by nuclear magnetic resonance spectroscopy (NMR). Thus, the polymerisation rate parameter (2fkp/〈k t〉1/2), along with the polymer stereoregularity, were obtained in terms of the molar fractions of meso and racemo diads and of syndiotactic, isotactic and heterotactic triads. The interaction of the polymers with cations was studied using polymer networks as solid phases in the solid-liquid extraction of lanthanide cations from both organic and aqueous media.

Preparation method of icotinib key intermediate

The invention discloses a preparation method of an icotinib key intermediate, and belongs to the technical field of drug synthesis. According to the preparation method, triethylene glycol(p-toluene sulfonate) and N-Boc-3,4-dihydroxyl aniline are used as raw materials; the raw materials carry out crown ether cyclization reaction, halogenation reaction and amination reaction (amidation reaction), quinoline cyclization reaction, and chlorination reaction to obtain an icotinib key intermediate, namely 4-chloro-quinazoline[6.7-6]-12-crown-4; the newly designed synthesis route does not need a strongacid solution, which is required by a conventional synthesis route; the dangerous operation is avoided, the generation of a large amount of acidic waste liquid is avoided; and the novel synthesis route has the advantages of simple operation and high yield.

Crown ether cyclic quinazoline compound, preparation method therefor and application thereof in preparing tumor therapy and imaging drug

The invention relates to a crown ether cyclic quinazoline derivative and medicinal salts thereof using in tumor therapy and imaging. The crown ether cyclic quinazoline compound is characterized in that a 2-, 3-, 4- substituted aniline is disposed at one end; a 6-, 7- substituted crown ether cyclic quinazoline structure is disposed at the other end; the substituent group R1 is located on the fourth-position aniline of a quinazoline mother ring and is 2-, 3-, 4- substituted alkoxy; and the crown ether cycle is located at the 6, 7 position of the mother ring, and is a 9-crown-3, 12-crown-4 and 15-crown-5, and the structural formula is formula I. The experimental result of antitumor activity in vitro of nonradioactive isotope labeling compounds shows that the compounds are good in inhibitory effect for four kind of cancer cells namely HepG2, A549, sy5y and DU145, and have the potential as cancer treatment medicine; and the body distribution experiment of 18F or 125I labeling compounds show that the compounds are higher in ingestion and certain detention in tumors and faster in blood clearance and have potential applied to tumor imaging.

Icotinib hydrochloride, synthesis, crystalline forms, pharmaceutical compositions, and uses thereof

The invention relates to 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, its therapeutic usage for treatment of diseases mediated by EGFR kinase and its combinatory therapeutic usage together with other therapeutic agents. The invention also provides synthetic methods for preparation of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride, its new crystalline forms, and the relevant synthetic intermediates for synthesis of 4-[(3-ethynylphenyl)amino]-6,7-benzo-12-crown-quinazoline hydrochloride.

HYDROCHLORIC ACID ICOTINIB, COMPOSITE, CRYSTALLOGRAPHIC FORM, COMBINED MEDICINE AND ITS APPLICATION

PROBLEM TO BE SOLVED: To provide a production method of a medicine which is an epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor, for treating and preventing excessive non-malignancy hyperplasia, pancreatitis, renal disease, cancer, arterialization or an angiogenesis-related disease of a mammal, or a medicine for germ cell transplantation of a mammal. SOLUTION: There is provided a use of 4-[(3-ethynyl phenyl)amino]-6-7-benzo-12-crown-hydrochloric acid quinazoline, illustrated by following formula, and these novel crystals (I, II, III, IV) for treatment of EGFR kinase-intermediating pathogen, and a use for treatment by joint use with another therapeutic agent. COPYRIGHT: (C)2015,JPO&INPIT