Icotinib (Hydrochloride)
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- CAS番号.
- 1204313-51-8
- 化学名:
- 别名:
- 英語名:
- Icotinib (Hydrochloride)
- 英語别名:
- CS-1906;CS-1016;Icotinib HCl;Icotinib (Hydrochloride);Icotinib (Hydrochloride) impurity;Icotinib Hydrochloride (BPI-2009);N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride;N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride Icotinib (Hydrochloride)
- CBNumber:
- CB22624183
- 化学式:
- C22H22ClN3O4
- 分子量:
- 427.89
- MOL File:
- 1204313-51-8.mol
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Icotinib (Hydrochloride) 物理性質
- 貯蔵温度 :
- Store at -20°C
- 溶解性:
- Soluble in DMSO
- 外見 :
- Powder
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
| 絵表示（GHS） |
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| 注意喚起語 |
警告 |
| 危険有害性情報 |
| コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
| H302 |
飲み込むと有害 |
急性毒性、経口 |
4 |
警告 |
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P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
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P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
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P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
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| 注意書き |
| P261 |
粉じん/煙/ガス/ミスト/蒸気/スプレーの吸入を避ける こと。 |
| P305+P351+P338 |
眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。 |
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Icotinib (Hydrochloride) 価格
| メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
Icotinib (Hydrochloride) 化学特性,用途語,生産方法
臨床応用
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.
合成
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.
Icotinib (Hydrochloride) 上流と下流の製品情報
原材料
準備製品
Icotinib (Hydrochloride) 生産企業
Global( 81)Suppliers
1204313-51-8()キーワード:
- 1204313-51-8
- Icotinib (Hydrochloride)
- N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride
- N-(3-Ethynylphenyl)-7,8,10,11,13,14-hexahydro-[1,4,7,10]tetraoxacyclododecino[2,3-g]quinazolin-4-amine hydrochloride Icotinib (Hydrochloride)
- Icotinib HCl
- CS-1016
- Icotinib Hydrochloride (BPI-2009)
- CS-1906
- Icotinib (Hydrochloride) impurity