カナグリフロジン水和物
カナグリフロジン水和物 物理性質
- 融点 :
- 94-96°C
- 貯蔵温度 :
- Hygroscopic, Refrigerator, under inert atmosphere
- 溶解性:
- DMSO（微量）、メタノール（微量）
- 外見 :
- 個体
- 色:
- ホワイトからオフホワイト
- 安定性：:
- 吸湿性
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） |
|
| 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 |
|
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。 |
|
カナグリフロジン水和物 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 |
カナグリフロジン水和物 化学特性,用途語,生産方法
効能
糖尿病治療薬, SGLT-2阻害薬
商品名
カナグル (田辺三菱製薬)
説明
Canagliflozin, an orally active and selective sodium–glucose
cotransporter 2 (SGLT2) inhibitor, was co-developed by
Mitsubishi Tanabe Pharma and Johnson & Johnson (J&J) for the
treatment of type 2 diabetes mellitus (T2DM) and obesity. The
drug was approved in March by the U.S. FDA and launched in
April 2013 in the U.S. SGLT2 is involved in the glucose re-absorption
pathway in the kidney, and its inhibition increases urinary
glucose excretion, and reduces plasma glucose and HbA1c levels.
In addition, canagliflozin is safe in combination with other commonly
used antidiabetic agents and has a significant effect on body
weight reduction. A recently published process patent from
ScinoPharm Taiwan describes the synthesis of canagliflozin.
使用
Canagliflozin Hemihydrate is a derivative of Canagliflozin (C175190), which is a sodium/glucose cotransporter 2 (SGLT2) inhibitor. Canagliflozin has been shown to dose dependently reduce calculated renal threshold for glucose excretion and increase urinary glucose excretion. Canagliflozin is a candidate for the treatment of type 2 diabetes and obesity.
合成
Synthesis of the aglycone region of canagliflozin was described
in a separate patent by first condensing commercially available 5-
bromo-2-methylbenzoyl chloride (14) and 2-(4-fluorophenyl)-
thiophene (15) under Friedel¨CCrafts acylation conditions to give
ketone 16 in 69% yield as a crystalline solid. Ketone 16 was then
reduced with triethylsilyl hydride in the presence of BF3Et2O at
low temperature to give aglycone bromide 17 in 70% yield. The
precursor for the glycoside moiety, commercially available glycoside
triol 18, was selectively treated with t-butyldiphenylsilyl
chloride (TBDPSCl) in THF in the presence of imidazole to give
the bis-silyl ether 19 in 81% yield. Next, a unique, stereospecific
b-C-arylglucosidation was developed to secure the union of the
aglyone- and glycoside-containing portions of canagliflozin.
Bromide 17 was subjected to magnesium powder under standard
Grignard conditions prior to treatment with AlCl3 in THF in situ.
This resulting mixture was then exposed to a solution of compound
19 in PhOMe which had been pre-treated with n-BuLi, and the entire mixture was then warmed to 150 ?? for 5 h to ultimately
give the b-anomer 20 in 56% yield. Finally, removal of the silyl
groups within 20 with tetrabutyl ammonium fluoride (TBAF) in
THF delivered canagliflozin hydrate (III) in 73% yield.
カナグリフロジン水和物 上流と下流の製品情報
原材料
準備製品
カナグリフロジン水和物 生産企業
Global( 268)Suppliers
カナグリフロジン水和物 スペクトルデータ(1HNMR)
928672-86-0(カナグリフロジン水和物)キーワード:
- 928672-86-0
- Canagliflozin hydrate (2:1)
- Canagliflozin heMihydrate
- D-Glucitol, 1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]Methyl]-4-Methylphenyl]-, hydrate (2:1)
- Canagliflozin heMihydrates
- (1S)-1,5-Anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol hydrate (2:1)
- Cageline
- Invokana hemihydrate
- JNJ 28431754 hemihydrate
- JNJ28431754 hemihydrate
- JNJ-28431754 hemihydrate
- JNJ28431754 HEMIHYDRATE; JNJ-28431754 HEMIHYDRATE; JNJ 28431754 HEMIHYDRATE; TA-7284 HEMIHYDRATE; TA7284 HEMIHYDRATE; INVOKANA HEMIHYDRATE
- TA7284 hemihydrate
- TA-7284 hemihydrate
- bis((2S,3R,4R,5S,6R)-2-(3-{[5-(4-fluorophenyl)thio phen-2-yl]methyl}-4-methylphenyl)-6-(hydroxymet hyl)oxane-3,4,5-triol) hydrate
- Canagliflozin (API)
- Canagli ozin Hemi hydrate
- (1S)-1,5-anhydro-1-C-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol Hemihydrate
- Canagliflozin hemihydrate (JNJ 28431754)
- TIANFU-CHEM 928672-86-0 Canagliflozin heMihydrate
- NSC 36678
- NSC 406879
- Cagliflozin heMihydrate
- (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol Hemihydrate
- Canagliflozin hydrate
- Kaglie net semihydrate
- (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol hydrate
- （１Ｓ）－１，５－アンヒドロ－１－（３－｛［５－（４－フルオロフェニル ）－２－チエニル］メチル｝－４－メチルフェニル）－Ｄ－グルシトール・１ ／２水和物
- カナグリフロジン水和物