JP5604568B2 - C−アリールグルコシドsglt2インヒビターおよび方法 - Google Patents
C−アリールグルコシドsglt2インヒビターおよび方法 Download PDFInfo
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Description
R1、R2およびR2aは個別に水素、OH、OR5、アルキル、CF3、OCHF2、OCF3、SR5iまたはハロゲン等であり;
R3およびR4は個別に水素、OH、OR5a、Oアリール、OCH2アリール、アルキル、シクロアルキル、CF3、-OCHF2、-OCF3、ハロゲン等である]
で示される化合物を開示している。これらの化合物はSGLT2輸送体のインヒビターであると報告されており、したがって糖尿病およびその合併症の処置のための方法を表す。
R3は水素、アルキルまたはアシル基[ここで、nは1-4である]であり、
R2は水素、アルキル、OH、NH2、ハロゲン、CO2Hまたはカルボキシイミド[ここで、kは1-4である]である]
で示される化合物を含み、これらは、とりわけ炎症性疾患、自己免疫疾患、感染症、癌、および癌の転移、再潅流障害、血栓症、潰瘍、創傷、骨粗鬆症、真性糖尿病およびアテローム性動脈硬化症の処置または予防に使用するために開示されている。
本発明に係る式Iの化合物は、以下の反応式およびその説明に示すようにして製造するが、ここで、温度は摂氏で表現する。
で示される化合物を、例えばH2O/THF/MeOHまたは水性MeOHまたは水性EtOHの1:2:3混合物のような溶媒中で、LiOHまたはNaOHのような塩基で処理することにより、図式1に示すようにして製造できる。
Ph = フェニル
Bn = ベンジル
t-Bu = 第三ブチル
Me = メチル
Et = エチル
TMS = トリメチルシリル
TBS = tert-ブチルジメチルシリル
THF = テトラヒドロフラン
Et2O = ジエチルエーテル
EtOAc = 酢酸エチル
DMF = ジメチルホルムアミド
MeOH = メタノール
EtOH = エタノール
i-PrOH = イソプロパノール
HOAcまたはAcOH = 酢酸
TFA = トリフルオロ酢酸
i-Pr2NEt = ジイソプロピルエチルアミン
Et3N = トリエチルアミン
DMAP = 4-ジメチルアミノピリジン
NaBH4 = 水素化硼素ナトリウム
n-BuLi = n-ブチルリチウム
Pd/C = 炭素上パラジウム
KOH = 水酸化カリウム
NaOH = 水酸化ナトリウム
LiOH = 水酸化リチウム
K2CO3 = 炭酸カリウム
NaHCO3 = 重炭酸ナトリウム
Ar = アルゴン
N2 = 窒素
min = 分
hまたはhr = 時間
L = リットル
mL = ミリリットル
μL = マイクロリットル
g = グラム
mg = ミリグラム
mol = モル
mmol = ミリモル
meq = ミリ当量
RT = 室温
satまたはsat'd = 飽和
aq. = 水性
TLC = 薄層クロマトグラフィー
HPLC = 高速液体クロマトグラフィー
LC/MS = 高速液体クロマトグラフィー/質量分析
MSまたはMass Spec = 質量分析
NMR = 核磁気共鳴
mp = 融点
ヒトSGLT2のmRNA配列(GenBank #M95549)をヒト腎臓mRNAからの逆転写と増幅により標準的分子生物技術を用いてクローニングした。このcDNA配列をCHO細胞に安定にトランスフェクトし、クローンを、本質上Ryan et al. (1994)に記載のようにしてSGLT2活性について検定した。クローン選択したセルラインにおけるSGLT2活性阻害の評価を、本質上Ryan et al.に記載のようにして、以下の改変を施して実施した。細胞を、F-12栄養混合物(HamのF-12)、10%牛胎児血清、300ug/mlゲネチシンおよびペニシリン-ストレプトマイシン中、96ウェル平板で、ウェル当たり75000または30000細胞になるまで2-4日間増殖させた。密集状態において細胞を10mM Hepes/Tris、pH7.4、137mM N-メチル-D-グルカミン、5.4mM KCl、2.8mM CaCl2、1.2mM MgSO4で2回洗浄した。次に、10mM Hepes/Tris、pH7.4、137mM NaCl、5.4mM KCl、2.8mM CaCl2、1.2mM MgSO4に入れた10μM[14C]AMG、および10μMインヒビター(最終的DMSO = 0.5%)と共に細胞を37℃で1.5時間インキュベートした。0.5mMフロリジンを含有する氷冷1X PBSで取り込み検定を停止させ、次いで細胞を0.1%NaOHで溶解した。MicroScintシンチレーション液を添加した後、細胞を1時間振盪し、次いでTopCountシンチレーションカウンターで[14C]AMGを定量した。NaCl有りおよび無しで対照実験を行った。EC50値の決定のため、適当な反応範囲で2 log間隔にわたり10のインヒビター濃度を使用し、3枚の平板を、平板にまたがって平均した。
塩化オキサリル(1.1mol)を含有するCH2Cl2 450mLに入れた市販の5-ブロモ-2-クロロ安息香酸(250g、1.06mol)の攪拌懸濁液にDMF 1.5mLを加えた。気体の活発な発生が止んだ後、反応を一夜攪拌し、次いでロータリーエバポレーターを用いて揮発成分を減圧除去した。この粗製5-ブロモ-2-クロロベンゾイルクロリドをCH2Cl2 200mLに溶解した後、この黄色溶液を、オーバーヘッドスターラーと内部温度計を取り付けた2Lの三頚フラスコに移した。攪拌した混合物を-3℃に冷却し、次いでフェネトール(130g、1.08mol)を加えた。温度が4゜を超えないよう、30分間かけて固体添加用漏斗からAlCl3(140g、1.07mol)を加えた。60%のAlCl3を加えた後に発生し始めた大量のHCl気体を、濃NaOH攪拌溶液中にこの気体を通すことによって捕捉した。添加終了の10分後にHPLCにより反応が95%完結していることが明らかとなった。混合物を4゜で1時間攪拌した後、氷上に注いで反応停止させた。続いてこの懸濁液をH2O(1L)で希釈し、CH2Cl2で3回抽出した。合した有機抽出物を1N HClで2回、H2Oで1回、1M NaOHで2回、そしてブラインで2回洗浄し、Na2SO4で乾燥した。揮発成分を除去した後、HPLCにより、残留物がオルト/パラ異性体の1:7混合物であることが分かった。無水EtOH 400mLから2回再結晶すると、5-ブロモ-2-クロロ-4'-エトキシベンゾフェノン230g(64%)が得られた。
1,2-ジクロロエタン/MeCNの1:2混合物900mLに入れたEt3SiH(400mL、2.51mol)および5-ブロモ-2-クロロ-4'-エトキシベンゾフェノン(390g、1.15mol)の10℃の攪拌溶液に、温度が20℃を超えないような速度でBF3・Et2O(150mL、1.58mol)を加えた。添加中、穏やかな発熱が続くよう留意されたい。20℃で一夜攪拌した後、HPLCにより反応が90%完結したことが分かった。さらにEt3SiH 40mLおよびBF3・Et2O 15mLを加えた後、反応を3時間50゜に加熱した。(高温は、Ritter反応の生成物N-アセチル5-ブロモ-2-クロロ-4'-エトキシジフェニルメチルアミンの生成を増加させることに注意)。冷却し、H2O 300mL中のKOH 120gで反応を停止させた。2時間攪拌した後、層を分離した。水層をCH2Cl2で2回抽出し;合した有機層を2M KOH 300mLで1回、相分離を助けるための10%ブラインを含有するH2Oで2回、そしてブラインで2回洗浄し、その後Na2SO4で乾燥した。揮発成分を除去した後、残留物を無水EtOH 400mLから再結晶すると、白色固体の5-ブロモ-2-クロロ-4'-エトキシジフェニルメタン230gが得られた。
THF 2.4Lに入れたグルコノラクトン(239g、1.34mol)およびN-メチルモルホリン(1180mL、10.73mol)の-5℃の攪拌溶液に、Ar雰囲気下で、温度が5℃を超えないような速度で滴下漏斗からトリメチルシリルクロリド(1022mL、8.05mol)を加えた。1時間後、この攪拌反応物を5時間35℃に加熱し、反応を一夜攪拌しながらこれを20℃に冷却した。トルエン3.6Lで希釈した後、混合物を0-5℃に冷却し、次いで温度が10℃を超えないような速度でH2O 7Lを注意深く加えた。最初のH2Oを添加した際に激しい発熱が起こることに注意されたい。混合後、相を分離させ、分割した。有機相を水性NaH2PO4(2L)、H2O(1L)、およびブライン(1L)で洗浄した。次に有機層をロータリーエバポレーターを用いて減圧濃縮し;得られた淡黄色油状物を2回トルエン250mLに溶解して再濃縮すると、標記化合物616gが得られた。
2:3:1のTHF/MeOH/H2O 480mLに入れたテトラアセチル化β-C-グルコシド(27.2g、49mmol)(E項に記載のようにして製造)の20゜の攪拌溶液にLiOH・H2O(2.3g、57mmol)を加えた。一夜攪拌した後、揮発成分をロータリーエバポレーターで除去した。残留物をEtOAc(300mL)に溶解した後、ブライン(150mL)で1回、5%水性KHSO4 10mLを含有するブライン(50mL)で1回、そして最後にブライン(50mL)で洗浄し、その後Na2SO4で乾燥した。揮発成分をロータリーエバポレーターを用いて除去し、得られた油状物を最少量のCH2Cl2に入れ減圧で泡状にすると、所望の標記C-アリールグルコシド20.4gが、0.11mol%のEtOAcを含有する硝子状オフホワイト色固体で得られた。
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US10/151,436 | 2002-05-20 | ||
US10/151,436 US6515117B2 (en) | 1999-10-12 | 2002-05-20 | C-aryl glucoside SGLT2 inhibitors and method |
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