ChemicalBook
Chinese english Germany Korea

オラパリブ

オラパリブ  化学構造式
763113-22-0
CAS番号.
763113-22-0
化学名:
オラパリブ
别名:
オラパリブ;オラパリブ (JAN)
英語化学名:
Olaparib
英語别名:
CS-1931;Azd2281;Olapani;KU 59436;Olaparid;Oraparib;Azd 2281;Azd-2281;Olaparib;Olaparibr
CBNumber:
CB02473811
化学式:
C24H23FN4O3
分子量:
434.46
MOL File:
763113-22-0.mol

オラパリブ 物理性質

比重(密度) :
1.43
酸解離定数(Pka):
12.07±0.40(Predicted)
CAS データベース:
763113-22-0

安全性情報

Rフレーズ  22-38-37-36
Sフレーズ  24/25-37/39
国連危険物分類  IRRITANT
HSコード  29339900

オラパリブ 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

オラパリブ 化学特性,用途語,生産方法

効能

抗悪性腫瘍薬, PARP阻害薬

商品名

リムパーザ (アストラゼネカ)

説明

Olaparib, marketed by AstraZeneca under the brand name Lynparza , was approved in the USA in December 2014 as a targeted, single-agent therapy for the treatment of germline BRCA-mediated advanced ovarian cancer.Olaparib, originally developed by KuDOS pharmaceuticals and later by AstraZeneca, functions as a poly ADP ribose polymerase inhibitor and has been specifically approved for patients who have received three or more treatments of chemotherapy. In clinical trials, the drug prolonged progression- free survival for patients suffering from platinum-sensitive recurrent serous ovarian cancer. Olaparib is also currently in various phases of investigation for treatment of breast, gastric, prostate, pancreatic and non-small cell lung cancer.

化学的特性

White Solid

使用

Olaparib is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Olaparib has been shown to induce significant killing of ATM-deficient lymphoid tumor cells in vitro and in vivo. Recent studies show that Olaparib increases radiosensitivity of a lung tumor xenograft, making it a potential candidate for use in combination with radiotherapy.

使用

Many of the products generated by alkylating agents on DNA can be efficiently repaired by normal base excision repair (BER). Some poly(ADP-ribose) polymerases (PARPs) assist in the repair of single-strand DNA nicks, an important step in BER. Olaparib is a potent inhibitor of PARP1 and PARP2 (IC50 = 5 and 1 nM, respectively) but is less effective against the PARP tankyrase-1 (IC50 = 1.5 μM). It can be used in cells and in animals, alone or in combination therapy with alkylating agents, to block BER and increase cancer cell death.[Cayman Chemical]

定義

ChEBI: A member of the class of N-acylpiperazines obtained by formal condensation of the carboxy group of 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid with the free amino group of N-(cyclpropylcarbonyl)pi erazine; used to treat advanced ovarian cancer.

Chemical Synthesis

This optimized synthesis begins with reaction of commercially available dimethyl phosphite and 2-carboxybenzaldehyde (201) to generate the corresponding phosphonate ester in 95% yield and 95% purity after aqueous workup.190 Addition of aldehyde 202 to this phosphonate ester intermediate in the presence of triethylamine led to formation of olefins 203a/203b in 96% yield as a 1:1 mixture of E/Z isomers. From olefins 203a/203b, a one-pot, three-step sequence was next performed to provide access to dihydrophthalazinyl acid 204. First, lactone ring-opening and nitrile hydrolysis was facilitated by reaction with aqueous sodium hydroxide under elevated temperatures, allowing for subsequent in situ formation of the corresponding dihydrophthalazine intermediate after addition of hydrazine hydrate. Acidification and precipitation of product with 2 N HCl led to isolation of the desired material in 77% yield and 96% purity after filtration. Further coupling of carboxylic acid 204 with Bocpiperazine (205) (HBTU, DIPEA, DMA) and subsequent removal of the carbamate with HCl/EtOH provided intermediate 206 in 46% yield from 204, relying on a pH-controlled workup procedure to enable isolation of material in high purity (94%) without requiring chromatography. The final step of the olaparib synthesis was completed via treatment of piperazine 206 with cyclopropane carbonyl chloride (207) and triethylamine, leading to isolation of olaparib in 90% yield and 99.3% purity after distillation.

オラパリブ 上流と下流の製品情報

原材料

準備製品


オラパリブ 生産企業

Global( 421)Suppliers
名前 電話番号 ファックス番号 電子メール 国籍 製品カタログ 優位度
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
+86-755-23284190 sales@tianpharm.com CHINA 305 58
Jurong Coupling Biotechnology Co., Ltd.
13656108824
coupling278191416@hotmail.com CHINA 184 58
PharmOrgSyn Laboratories Co., Ltd.
13916602830 021-38228826
david.rao@pharmorgsyn.com CHINA 128 58
HONG KONG IPURE BIOLOGY CO.,LIMITED
18062405514 86 18062405514
ada@ipurechemical.com CHINA 3475 58
Capot Chemical Co.,Ltd.
+86(0)13336195806 +86-571-85586718
+86-571-85864795 sales@capotchem.com China 20012 60
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Hi-Tech Chemistry Corp
0519-86626038
yuhh@hitechem.com CHINA 811 58
Shanghai Bojing Chemical Co.,Ltd.
+86-21-37122233
+86-21-37127788 Candy@bj-chem.com CHINA 497 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8909 55

763113-22-0(オラパリブ )キーワード:


  • 763113-22-0
  • 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)Methyl]-2-fluorobenzoyl]piperazin
  • Olaparid AZD2281
  • 4-(3-(4-(Cyclopropanecarbonyl)piperazine-1-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
  • 4-[[3-[[4-(Cyclopropylcarbonyl)-1-piperazinyl]carbonyl]-4-fluorophenyl]Methyl]-1(2H)-phthalazinone
  • KU 59436
  • AZD2281(olaparib)/AZD-2281
  • AZD2281(olaparib)
  • 4-(3-(1-(cyclopropanecarbonyl)piperazine-4-carbonyl)-4-fluorobenzyl)phthalazin-1(2H)-one
  • Olaparib-D8
  • Olaparib, 99%, PARP inhibitor
  • AZD 2281 - Olaparib | KU 0059436
  • AZD2281; KU-0059436; KU0059436; AZD-2281; KU0059436; AZD 2281
  • CS-1931
  • (937799-91-2) olaparib
  • AZD2281,?Ku-0059436
  • Olaparib (AZD2281, Ku-0059436)
  • Olaparid
  • Olaparib 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine
  • Olaparib, >=98%
  • 4-[(3-[(4-cyclopropylcarbonyl)piperazin-4-yl]carbonyl) -4-fluorophenyl]methyl(2H)phthalazin-1-one
  • Oraparib
  • 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]pipera
  • Azd 2281
  • Azd2281
  • Azd-2281
  • Ku-0059436
  • 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one Olaparib
  • 4-[3-(4-Cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one
  • Olaparib
  • 1-(Cyclopropylcarbonyl)-4-[5-[(3,4-dihydro-4-oxo-1-phthalazinyl)methyl]-2-fluorobenzoyl]piperazine
  • オラパリブ
  • オラパリブ (JAN)
Copyright 2017 © ChemicalBook. All rights reserved