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1204313-51-8

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1204313-51-8 Usage

Clinical Use

Icotinib hydrochloride, developed by the Chinese pharmaceutical company Zhejiang Bata Pharma Inc., is a potent small molecule epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor for the treatment of non-small cell lung cancer (NSCLC). It was first approved by the SFDA of China, and launched under the brand name Conmana in the middle of 2011, representing an important milestone for Chinese pharmaceutical research and development. As the third EGFR-TKI drug targeting NSCLS therapy, icotinib hydrochloride possesses a similar structure to gefitinib (Iressa, AstraZeneca) and erlotinib (Tarceva, OST & Roche). Interestingly, a randomized, double-blind phase III clinical study of icotinib versus gefitinib in 399 patients with advanced NSCLC demonstrated that icotinib provides similar efficacy to gefitinib, but with better tolerability in NSCLC patients previously treated with one or two chemotherapy agents.

Synthesis

Icotinib was prepared by a similar process approach to that of erlotinib. Beginning from commercially available 2,20-(ethylenedioxy)diethanol (162), bis-tosylation to 163, followed by bis-alkylation with commercially available catechol derivative 164 provided crown-4-ether 165 in 96% yield. Nitration of polyether 165 using concentrated nitric acid and concentrated sulfuric acid provided nitroarene 166 in 65% yield. Reduction of the nitroarene under catalytic hydrogenation conditions gave amine 167 in 85% yield. Condensation of the amine 167 with formamide in the presence of ammonium formate afforded quinazolinone 168 in 80% yield. The chlorination of 168 using POCl3 furnished quinazolyl chloride 169 in 77% yield. The treatment of chloride 169 with amine 170 followed by the HCl salt formation produced icotinib hydrochloride (XIV) in good yield.

Check Digit Verification of cas no

The CAS Registry Mumber 1204313-51-8 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,2,0,4,3,1 and 3 respectively; the second part has 2 digits, 5 and 1 respectively.
Calculate Digit Verification of CAS Registry Number 1204313-51:
(9*1)+(8*2)+(7*0)+(6*4)+(5*3)+(4*1)+(3*3)+(2*5)+(1*1)=88
88 % 10 = 8
So 1204313-51-8 is a valid CAS Registry Number.

1204313-51-8SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 17, 2017

Revision Date: Aug 17, 2017

1.Identification

1.1 GHS Product identifier

Product name Icotinib Hydrochloride

1.2 Other means of identification

Product number -
Other names UNII-JTD32I0J83

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:1204313-51-8 SDS

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