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ジプラシドン塩酸塩一水和物

ジプラシドン塩酸塩一水和物 化学構造式
138982-67-9
CAS番号.
138982-67-9
化学名:
ジプラシドン塩酸塩一水和物
别名:
ジプラシドン塩酸塩一水和物;5-[2-[4-(1,2-ベンゾイソチアゾール-3-イル)-1-ピペラジニル]エチル]-6-クロロ-1,3-ジヒドロ-2H-インドール-2-オン塩酸塩一水和物;ジプラシドン塩酸塩;ZIPRASIDONE 塩酸塩 一水和物;ジプラシドン塩酸塩水和物;ジプラシドン塩酸塩水和物 (JAN)
英語化学名:
5-[2-[4-(1,2-Benzisothiazol-3yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one hydrochloride
英語别名:
CP-88059-1;Ziprasidong Hcl;ZIPRASIDONE HCL;Ziprasidone HCl hydrate;ZIPRASIDONE INTERMEDIATE;ZIPRASIDONE HYDROCHLORIDE;ZIPRASIDONE HCL MONOHYDRATE;ZIPRASITONE HCl MONOHYDRATE;Geodon Hydrochloride Hydrate;Ziprasidone Hydrochloride (200 mg)
CBNumber:
CB0166832
化学式:
C21H24Cl2N4O2S
分子量:
467.41186
MOL File:
138982-67-9.mol

ジプラシドン塩酸塩一水和物 物理性質

融点 :
300°C
貯蔵温度 :
2-8°C
溶解性:
DMSO: >10mg/mL
外見 :
solid
Merck :
14,10171
CAS データベース:
138982-67-9(CAS DataBase Reference)
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)
Sフレーズ  24/25
RIDADR  UN1230 - class 3 - PG 2 - Methanol, solution
WGK Germany  3
RTECS 番号 NM3241200
HSコード  38220010
絵表示(GHS)
注意喚起語 Warning
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
H317 アレルギー性皮膚反応を起こすおそれ 感作性、皮膚 1 警告 P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H373 長期にわたる、または反復暴露により臓器の障 害のおそれ 特定標的臓器有害性、単回暴露 2 警告 P260, P314, P501
注意書き
P260 粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。
P280 保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。
P333+P313 皮膚刺激または発疹が生じた場合:医師の診断/手当てを 受けること。

ジプラシドン塩酸塩一水和物 価格 もっと(22)

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
富士フイルム和光純薬株式会社(wako) W01TOC3085 ジプラシドン塩酸塩
Ziprasidone hydrochloride
138982-67-9 10mg ¥38000 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01TOC3085 ジプラシドン塩酸塩
Ziprasidone hydrochloride
138982-67-9 50mg ¥162000 2018-12-26 購入
東京化成工業 Z0032 ジプラシドン塩酸塩一水和物 >98.0%(HPLC)
Ziprasidone Hydrochloride Monohydrate >98.0%(HPLC)
138982-67-9 50mg ¥3300 2021-03-23 購入
東京化成工業 Z0032 ジプラシドン塩酸塩一水和物 >98.0%(HPLC)
Ziprasidone Hydrochloride Monohydrate >98.0%(HPLC)
138982-67-9 250mg ¥11000 2021-03-23 購入
Sigma-Aldrich Japan Y0001286 European Pharmacopoeia (EP) Reference Standard
Ziprasidone hydrochloride monohydrate European Pharmacopoeia (EP) Reference Standard
138982-67-9 ¥35200 2021-03-23 購入

ジプラシドン塩酸塩一水和物 化学特性,用途語,生産方法

外観

白色~黄赤色~緑色粉末~結晶

用途

Na+ /H+ 交換輸送体アイソフォーム 1(NHE1)阻害剤です。MMP2/9 の活性を阻害します。

用途

5-HT2A/D2 受容体アンタゴニ ストです。

用途

5-HT2A/D2 受容体アンタゴニストです。非定型抗精神病作用を示します。

効能

統合失調症治療薬

化学的特性

Pale Tan Powder

Originator

Geodon,Pfizer,USA

使用

Ziprasidone Hydrochloride is the hydrochloride salt of a benzisothiazolylpiperazine analog structurally related to the atypical antipsychotic drug tiospirone that antagonizes both central serotonin 5-HT2A (Ki = 0.42 nM) and dopamine D2 (Ki = 4.8 nM) receptors. It is also a potent agonist at 5-HT1A receptors (Ki = 3.4 nM), increasing cortical dopamine release which may offset negative effects associated with dopamine D2 antagonism, and an inverse agonist at 5-HT1B and 5-HT1D receptors (pKis = 8.8 and 8.6, respectively).[Cayman Chemical]

使用

Combined serotonin (5HT2) and dopamine (D2) receptor antagonist. Used as an antipsychotic.

使用

antipsychotic;Dopamine D2/serotonin 5-HT2 antagonist

定義

ChEBI: The hydrochloride hydrate salt of ziprasidone.

Manufacturing Process

Preparation of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro- 1,3-dihydro-2H-indol-2-one
A 20-gallon glass lined tank, under a nitrogen atmosphere, was charged with 33.5 liters of water and 9.4 kilograms (kg) of sodium carbonate (dense, 89.1 moles, 3.4 eq.). The resulting mixture was stirred to give a solution. To the solution 6.4 kg of 2-chloroethyl-6-chloro-oxindole (27.8 moles, 1.06 eq.) was charged, followed by 6.7 kg of 3-piperazinyl-1,2-benzisothiazole hydrochloride (26.2 moles, 1.0 eq.). This was stirred and heated to reflux (100°C). After 11 hours the reaction was sampled for high pressure liquid chromatography (HPLC) assay. The reflux was continued for another 2 hours then the reaction was cooled to 25°C and the slurry stirred for 1 hour. The product was observed and found to be essentially free from lumps and gummy matter. The product was collected by filtration. A 14 liter water was added to the tank and cooled to 12°C and then used to wash the product. The cake was pulled as dry as possible, and the product was returned to the tank along with 40 liters of isopropyl alcohol (IPO). This was cooled and then stirred for 2 hours and the product was collected by filtration. The cake was washed with 13.4 liters of fresh IPO, then dried under vacuum at 30° to 40°C. After drying, 17.3 kg of the title compound was obtained. This was in excess of the theoretical weight yield due to some residual carbonate in the crude product.
Recrystallization of 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6- chloro-1,3-dihydro-2H-indol-2-one
To a clean and dry 100-gallon glass lined tank was charged 9.0 kg of the material obtained above and 86 gallons of tetrahydrofuran (THF). The slurry was heated to reflux and held for 1 hour. The hazy solution was then filtered through a 14" sparkler precoated with filter aid and backed with a Fulflo filter to a clean, dry, and "spec free" glass-lined tank on a lower level. The batch was concentrated by vacuum distillation. Another 8.3 kg of the material obtained in above was dissolved in 83 gallons of THF in the upper tank. This was filtered to the lower tank. The tank lines and sparkler were rinsed with 10 gallons of THF. The batch was concentrated to about 22 gallons, then cooled to 5°C and stirred for 1 hour. The product was collected by filtration. Then 20 gallons of fresh IPO were cooled in the tank and used to rinse the product cake. The product was collected and dried under vacuum at 45°C; yielding 9.05 kg of product (83.8% yield for the coupling and recrystallization. The product matched the spectra of a standard NMR and showed the correct retention time by HPLC with 99.7% assay. Another way for preparation of 5-(2-(4-(1,2-benzisothiazol-3-yl)-piperazinyl)ethyl)-6-chloro-1,3-dihydro-2-H- indol-2-one.
A clean and dry 20-gallon glass lined tank was charged with 19 L of water and 4.44 kg of sodium carbonate, after the carbonate had dissolved 4.29 kg (17.5 moles) of 5-(2-chloroethyl)-6-chloro-oxindole and 3.62 kg (16.5 moles) of 1- (1,2-benzisothiazol-3-yl)piperazine were added. The aqueous slurry was heated to reflux and the temperature maintained for 14 hours. When the reaction was complete the solution was cooled to 20°C and filtered. The wet product was reslurried in 23 L of isopropyl alcohol at room temperature for 2 hours. The product was collected by filtration on 2 large Buchner funnels, each was washed with 3.4 L of fresh isopropyl alcohol. The product was vacuum dried at 30° to 40°C. until no isopropyl alcohol remained, giving 5.89 kg (86.4% yield) of the desired free base which matched a standard sample by high performance liquid chromatography (HPLC).
A clean and dry 20-gallon reactor was charged with 17.4 gallons of deionized water and 4.44 L of concentrated hydrochloric acid, to give a 0.77 M solution. To the solution was added 4.44 kg of the anhydrous 5-(2-(4-(1,2- benzisothiazol-yl)-1-piperazinyl)-ethyl)-6-chloro-1,3-dihydro-2H-indol-2-one free base. The slurry was warmed to 65°C and held for 18 hours. The slurry was cooled to room temperature. The product was filtered and washed with 2x5-gallon portions of deionized water, and then air dried at 50°C for 30 hours. The dried product contained 4.4% water and the x-ray diffraction method confirmed that the desired product was obtained.

brand name

Geodon (Pfizer).

Therapeutic Function

H-Indol-2-one, 5-(2-(4-(1,2-benzisothiazol-3-yl)-1- piperazinyl)ethyl)-6-chloro-1,3-dihydro-, monohydrochloride monohydrate

生物活性

Atypical antipsychotic that displays combined serotonin and dopamine receptor antagonism. Displays high affinity at 5-HT 2A receptors with a 5-HT 2A /D 2 affinity ratio greater than any other clinically available atypical antipsychotics (pK i values are 9.38, 8.88, 8.69, 8.47, 8.32, 8.14, 7.98, 7.49, 7.33 and 6.28 for 5-HT 2A , 5-HT 2C , 5-HT 1D , 5-HT 1A , D 2 , D 3 , α 1 , D 4 , H 1 and D 1 receptors respectively).

Biochem/physiol Actions

Ziprasidone is an atypical antipsychotic; FDA approved for the treatment of schizophrenia.

ジプラシドン塩酸塩一水和物 上流と下流の製品情報

原材料

準備製品


ジプラシドン塩酸塩一水和物 生産企業

Global( 259)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
Henan DaKen Chemical CO.,LTD.
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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 9115 55
career henan chemical co
+86-0371-55982848
sales@coreychem.com China 29954 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 linda@hubeijusheng.com CHINA 28229 58
Xiamen AmoyChem Co., Ltd
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BOC Sciences
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Chongqing Chemdad Co., Ltd
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Alchem Pharmtech,Inc.
8485655694
sales@alchempharmtech.com United States 63726 58
CONIER CHEM AND PHARMA LIMITED
86-18523575427
sales@conier.com China 47498 58

138982-67-9(ジプラシドン塩酸塩一水和物)キーワード:


  • 138982-67-9
  • Ziprasidone (hydrochloride hydrate)
  • 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one hydrochloride hyd
  • Ziprasidone for system suitability 2
  • Ziprasidone for system suitability 1
  • ZIPRASIDONE HCL
  • ZIPRASIDONE HYDROCHLORIDE
  • ZIPRASIDONE HYDROCHLORIDE MONOHYDRATE
  • 5-[2-[4-(1,2-BENZISOTHIAZOL-3YL)-1-PIPERAZINYL]ETHYL]-6-CHLORO-1,3-DIHYDRO-2H-INDOL-2-ONE, HYDROCHLORIDE MONOHYDRATE
  • CP-88059-1
  • 5-[2-[4-(1,2-benzisothiazol-3yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2h-indol-2-one hydrochloride
  • Ziprasidong Hcl
  • 5-[2-[4-(1,2-Benzisothiazol-3yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one, Hydrochloride Monohydrate, CP-88059-1
  • 2H-Indol-2-one, 5-2-4-(1,2-benzisothiazol-3-yl)-1-piperazinylethyl-6-chloro-1,3-dihydro-, monohydrochloride, monohydrate
  • ZIPRASIDONE INTERMEDIATE
  • ZIPRASIDONE HCL MONOHYDRATE
  • ZIPRASITONE HCl MONOHYDRATE
  • CP-88059, Geodon, 5-[2-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-2H-indol-2-one monohydrate hydrochloride
  • Ziprasidone monohydrate hydrochloride
  • 5-[2-[4-(1,2-Benzisothiazol-3-y1)-1-piperazinyl]ethyl]-6-chlom-1,3-dihydro-2H-indol-2-one
  • 2H-Indol-2-one, 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6-chloro-1,3-dihydro-, hydrochloride, hydrate (1:1:1)
  • Ziprasidone Hydrochloride Monohydrate Also see: G364400
  • Ziprasidone Hydrochloride (200 mg)
  • Geodon Hydrochloride Hydrate
  • 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one hydrochloride hydrat
  • Ziprasidone Hydrochloride Mohydrate
  • Ziprasidone hydrochloride monohydrate, 99%, a novel and potent dopamine and serotonin (5-HT) receptor antagonist
  • 5-(2-(4-(Benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one hydrochloride hydrate
  • 5-(2-(4-(1,2-Benzisothiazol-3-yl)Piperazin-1-yl)Ethyl)-6-Chloroindolin-2-One Hydrochloride Hydrate
  • Ziprasidone HCl hydrate
  • Ziprasidone hydrochloride monohydrate CRS
  • ジプラシドン塩酸塩一水和物
  • 5-[2-[4-(1,2-ベンゾイソチアゾール-3-イル)-1-ピペラジニル]エチル]-6-クロロ-1,3-ジヒドロ-2H-インドール-2-オン塩酸塩一水和物
  • ジプラシドン塩酸塩
  • ZIPRASIDONE 塩酸塩 一水和物
  • ジプラシドン塩酸塩水和物
  • ジプラシドン塩酸塩水和物 (JAN)
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