トホグリフロジン水和物
トホグリフロジン水和物 物理性質(zhì)
- 貯蔵溫度 :
- Store at -20°C
- 溶解性:
- DMF: 30 mg/ml; DMSO: 30 mg/ml; Ethanol: 30 mg/ml; Ethanol:PBS (pH7.2)(1:20): 0.05 mg/ml
- 外見 :
- A crystalline solid
- 色:
- White to off-white
- InChIKey:
- ZXOCGDDVNPDRIW-XGKWJGTMNA-N
- SMILES:
- O[C@@H]1[C@H]([C@H](O)[C@@H](CO)O[C@@]21OCC1=CC=C(CC3C=CC(CC)=CC=3)C=C21)O.O |&1:1,2,3,5,9,r|
安全性情報(bào)
- リスクと安全性に関する聲明
- 危険有害性情報(bào)のコード(GHS)
| 絵表示（GHS） |
|
| 注意喚起語 |
警告 |
| 危険有害性情報(bào) |
| コード |
危険有害性情報(bào) |
危険有害性クラス |
區(qū)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 |
|
P264, P270, P301+P312, P330, P501 |
| H315 |
皮膚刺激 |
皮膚腐食性/刺激性 |
2 |
警告 |
|
P264, P280, P302+P352, P321,P332+P313, P362 |
| H319 |
強(qiáng)い眼刺激 |
眼に対する重篤な損傷性/眼刺激 性 |
2A |
警告 |
|
P264, P280, P305+P351+P338,P337+P313P |
| H335 |
呼吸器への刺激のおそれ |
特定標(biāo)的臓器毒性、単回暴露； 気道刺激性 |
3 |
警告 |
|
|
|
| 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(chǎng)合：水で數(shù)分間注意深く洗うこと。次にコ ンタクトレンズを著用していて容易に外せる場(chǎng)合は外す こと。その後も洗浄を続けること。 |
|
トホグリフロジン水和物 価格
| メーカー |
製品番號(hào) |
製品説明 |
CAS番號(hào) |
包裝 |
価格 |
更新時(shí)間 |
購入 |
トホグリフロジン水和物 化學(xué)特性,用途語,生産方法
効能
糖尿病治療薬, SGLT-2阻害薬
商品名
アプルウェイ (サノフィ); デベルザ (興和)
説明
Tofogliflozin hydrate, which is a sodium-glucose co-transporter
2 inhibitor, was approved in Japan for the treatment of type 2 diabetes
at the same time as luseogliflozin hydrate (XIX). The drug
was discovered by Chugai Pharmaceutical and jointly developed
with Sanofi-Aventis and Kowa. Tofogliflozin hydrate reduces
glucose levels by inhibiting the reuptake of glucose by selectively
inhibiting SGLT2, and plays a key role in the reuptake of glucose
in the proximal tubule of the kidneys.
合成
Reduction of commercially available 2-bromoterephtalic acid
(268) through the use of trimethoxyborane and borane-
THF proceeded in 89% yield to afford diol 269. Subjection of
this compound to 2-methoxypropene (270) under acidic
conditions generated bis-acetonide 271. This bromide then
underwent lithium¨Chalogen exchange followed by exposure to
magnesium bromide and treatment with lactone 272 (which
was prepared by persilylation of commercially available
(3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2Hpyran-
2-one (277). This mixture was worked up with
aqueous ammonium chloride and upon treatment with p-TsOH
in methanol resulted in spiroacetal 273. Next, global protection
of all alcohol functionalities within 273 was affected by reaction
with methylchloroformate and DMAP in acetonitrile. The benzyl
carbonate within 274 was selectively exchanged via Suzuki coupling
with 4-ethylphenylboronic acid (275) to afford methylene
dibenzyl system 276. Subsequent treatment with aqueous sodium
hydroxide in methanol followed by crystallization from 1:6 acetone
and water furnished the desired product tofogliflozin hydrate
(XXXIV) in 75% yield.
トホグリフロジン水和物 上流と下流の製品情報(bào)
原材料
準(zhǔn)備製品
トホグリフロジン水和物 生産企業(yè)
Global( 129)Suppliers
トホグリフロジン水和物 スペクトルデータ(1HNMR)
1201913-82-7(トホグリフロジン水和物)キーワード:
- 1201913-82-7
- Tofogliflozin (hydrate)
- (1S,3'R,4'S,5'S,6'R)-6-[(4-Ethylphenyl)methyl]-3',4',5',6'-tetrahydro-6'-(hydroxymethyl)spiro[isobenzofuran-1(3H),2'-[2H]pyran]-3',4',5'-triol hydrate (1:1)
- Tofogliflozin hydrate (1:1)
- Tofogliflozin hydrate (1:1)-API
- Tofogliflozin anyhydrous
- UNII-554245W62TTofogliflozin [INN]
- CSG 452(hydrate)
- (3S,3'R,4'S,5'S,6'R)-5-[(4-ethylphenyl)methyl]-6'-(hydroxymethyl)spiro[1H-2-benzofuran-3,2'-oxane]-3',4',5'-triol,hydrate
- Tofogliflozin(CSG452)
- Tofogliflozin Hydrate (JAN)
- Tofogliflozin hydrate (CSG-452 hydrate)
- TOFOGLIFLOZIN USP/EP/BP
- Tofogliflozin Monohydrate
- CSG452; CSG-452; TOFOGLIFLOZIN; CSG 452; UNII-554245W62TTOFOGLIFLOZIN [INN]; TOFOGLIFLOZIN ANYHYDROUS
- Togliflozin
- Tofogliflozin Monohydrate（CSG 452 hydrate）
- (1S,3'R,4'S,5'S,6'R)-6-(4-Ethylbenzyl)-6'-(hydroxymethyl)-3',4',5',6'-tetrahydro-3H-spiro[isobenzofuran-1,2'-pyran]-3',4',5'-triol hydrate
- Tofogliflozin (hydrate), 10 mM in DMSO
- (1S,3'R,4'S,5'S,6'R)-6-(4-Ethylbenzyl)-6'-(hydroxymethyl)-3',4',5',6'-tetrahydro-3H-spiro[isobenzofuran-1,2'-pyran]-3',4',5'-triol hydrate
- トホグリフロジン水和物
- トホグリフロジン水和物 (JAN)