JP5766661B2 - キラル8−(3−アミノ−ピペリジン−1−イル)−キサンチンの製造方法 - Google Patents
キラル8−(3−アミノ−ピペリジン−1−イル)−キサンチンの製造方法 Download PDFInfo
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Description
の8-(3-アミノピペリジン-1-イル)-キサンチンは国際特許出願WO 02/068420、WO04/018468、WO04/018467、WO2004/041820及びWO2004/046148から既に知られており、これらには有益な薬理学的性質(特に酵素ジペプチジルペプチダーゼIV(DPP-IV)の活性に対する抑制作用を含む)を有する化合物が記載されている。それ故、この型の化合物は増大されたDPP-IV活性と関連し、又は特に真性糖尿病型Iもしくは型II、前糖尿病、又はグルコーストレランスの低下の、DPP-IV活性の低下により予防もしくは軽減し得る障害又は症状を予防又は治療するのに適している。
WO04/018468は8-(3-アミノピペリジン-1-イル)-キサンチンが一般式(II)の相当するtert.-ブチルオキシカルボニル保護誘導体を脱保護することにより調製される調製方法を開示している。
本発明の方法によれば、適当なキサンチン前駆体(III)がスキーム1に従って好適な溶媒中で20〜160℃、好ましくは8〜140℃の温度で鏡像体上純粋な、又はラセミの3-(フタルイミド)ピペリジンと反応させられる。使用される溶媒は、例えば、テトラヒドロフラン(THF)、ジオキサン、N,N-ジメチルホルムアミド(DMF)、ジメチルアセトアミド(DMA)、N-メチル-2-ピロリドン(NMP)又はジメチルスルホキシド(DMSO)であってもよい。NMPを使用することが好ましい。続いて、フタリル保護基がそれ自体知られている方法により取り外される。可能な取り外し方法が、例えば、T.W. Greene著“有機合成における保護基”, Wiley 1981 265頁に記載されている(例えば、エタノール中のヒドラジン)。
Xはハロゲン、例えば、フッ素原子、塩素原子もしくは臭素原子、又はスルホン酸エステル、例えば、フェニルスルホニルオキシ基、p-トルエンスルホニルオキシ基、メチルスルホニルオキシ基もしくはトリフルオロメチルスルホニルオキシ基の群から選ばれた脱離基であり、
R1はフェニルカルボニルメチル基、ベンジル基、ナフチルメチル基、ピリジニルメチル基、ピリミジニルメチル基、キノリニルメチル基、イソキノリニルメチル基、キナゾリニルメチル基、キノキサリニルメチル基、ナフチリジニルメチル基又はフェナントリジニルメチル基であり、その芳香族部分又はヘテロ芳香族部分は夫々の場合にRaにより一置換又は二置換されており、これらの置換基は同じであってもよく、また異なっていてもよく、かつ
Raは水素原子、フッ素原子、塩素原子もしくは臭素原子又はシアノ基、メチル基、トリフルオロメチル基、エチル基、フェニル基、メトキシ基、ジフルオロメトキシ基、トリフルオロメトキシ基もしくはエトキシ基であり、又は
二つのRa基は、それらが隣接炭素原子に結合されている場合には、また-O-CH2-O-基もしくは-O-CH2-CH2-O-基であってもよく、
R2はメチル基、エチル基、プロピル基、イソプロピル基、シクロプロピル基又はフェニル基であり、かつ
R3は2-ブテン-1-イル基、3-メチル-2-ブテン-1-イル基、2-ブチン-1-イル基、2-フルオロベンジル基、2-クロロベンジル基、2-ブロモベンジル基、2-ヨードベンジル基、2-メチルベンジル基、2-(トリフルオロメチル)ベンジル基又は2-シアノベンジル基である。
Xが塩素原子又は臭素原子であり、
R1がフェニルカルボニルメチル基、ベンジル基、ナフチルメチル基、ピリジニルメチル基、ピリミジニルメチル基、キノリニルメチル基、イソキノリニルメチル基、キナゾリニルメチル基、キノキサリニルメチル基又はナフチリジニルメチル基であり、その芳香族部分又はヘテロ芳香族部分が夫々の場合にRaにより一置換又は二置換されており、これらの置換基は同じであってもよく、また異なっていてもよく、かつ
Raが水素原子、フッ素原子もしくは塩素原子又はシアノ基、メチル基、エチル基、メトキシ基もしくはエトキシ基であり、
R2がメチル基、エチル基、プロピル基、イソプロピル基、シクロプロピル基又はフェニル基であり、かつ
R3が2-ブテン-1-イル基、3-メチル-2-ブテン-1-イル基、2-ブチン-1-イル基、2-フルオロベンジル基、2-クロロベンジル基、2-ブロモベンジル基、2-ヨードベンジル基、2-メチルベンジル基、2-(トリフルオロメチル)ベンジル基又は2-シアノベンジル基である、これらの化合物について好ましい。
その方法は
Xが塩素原子又は臭素原子であり、
R1がシアノベンジル基、(シアノピリジニル)メチル基、キノリニルメチル基、(メチルキノリニル)メチル基、イソキノリニルメチル基、(メチルイソキノリニル)メチル基、キナゾリニルメチル基、(メチルキナゾリニル)メチル基、キノキサジニルメチル基、(メチルキノキサリニル)メチル基、(ジメチルキノキサリニル)メチル基又はナフチリジニルメチル基であり、
R2がメチル基、シクロプロピル基又はフェニル基であり、かつ
R3が2-ブテン-1-イル基、3-メチル-2-ブテン-1-イル基、2-ブチン-1-イル基、2-クロロベンジル基、2-ブロモベンジル基又は2-シアノベンジル基である、これらの化合物について、特に化合物1-〔(4-メチルキナゾリン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノピペリジン-1-イル)-キサンチン、1-〔(3-メチルイソキノリン-1-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-((R)-3-アミノピペリジン-1-イル)-キサンチン及び1-〔(3-シアノピペリジン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノピペリジン-1-イル)-キサンチンについて更に好ましく、この場合、Xは臭素である。
夫々の場合に、(R)-3-(フタルイミド)ピペリジンを試薬として使用することが好ましい。式(III)の化合物の調製が既に先に引用された文献に記載されており、それ自体知られている方法により行なわれる。
式(IV)の化合物のこの極めて簡単な鏡像体分離は当業者にとって驚くべきである。水素化反応からのラセミ塩基はこの目的のために前もって精製される必要はない。その方法は工業規模でさえも問題なく実施できる。
加えて、3-アミノピペリジンと無水フタル酸の予期しない程にきれいな反応はそれ自体驚くべきである。何とならば、文献(例えば、米国特許第4,005,208号、特に実施例27)によれば、所望の生成物に加えて、環窒素原子がアシル化されている誘導体を含む混合物が予想されるからである。
a.水素化
その反応はまた苛酷ではない圧力で進行する。
b.アシル化
c.光学分割
d.再結晶
溶液が生成するまで湿った粗生成物をアセトン50リットル及び水90リットルの混合物中で加熱、還流する。続いて、その溶液を5℃に冷却し、その経過中に生成物が結晶化する。その懸濁液を5℃で30分間撹拌し、生成物を遠心分離し、最後にアセトン20リットル及び水10リットルの混合物で洗浄する。その混合物を不活性下で乾燥キャビネット中で45℃で乾燥させる。
収量:11.7-12.5kg(理論値の29-31%)
a.2-クロロメチル-4-メチルキナゾリン
1時間以内に添加する。供給容器を1.4-ジオキサン2リットルでフラッシする。その後に、反応器内容物を6℃に温め、更に約2時間撹拌する。
更なる反応器に最初に水122リットル及び水酸化ナトリウム溶液(50%)62.04kg(775.31モル)の混合物を仕込み、6℃に冷却する。最初の反応器からの反応混合物を少しづつ添加する。内部温度は11℃以下である。続いて、最初の反応器を最初に1,4-ジオキサン6リットル、次いで水6リットルでフラッシする。得られる懸濁液を5℃で更に30分間撹拌する。生成物を遠心分離し、水41リットルで洗浄し、不活性下で乾燥キャビネット中で35℃で乾燥させる。
収量:10.5-12.1kg(理論値の74-85%)
b.1-〔(4-メチルキナゾリン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-ブロモキサンチン
収量:11.6-12.6kg(理論値の76-83%)
c.1-〔(4-メチルキナゾリン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-フタルイミドピペリジン-1-イル)-キサンチン
収量:12.0-12.5kg(理論値の90-94%)
d.1-〔(4-メチルキナゾリン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノピペリジン-1-イル)-キサンチン
収量:1174g(理論値の83.2%)
工程dの別法
1-〔(4-メチルキナゾリン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-フタルイミドピペリジン-1-イル)-キサンチン1400g(2.32モル)を最初にテトラヒドロフラン4.9リットルに仕込み、続いて55-65℃に加熱する。続いて、水350ml及びエタノールアミン1433g(2.32モル)をその懸濁液に添加する。その反応を完結するために、その混合物を60-63℃で更に3時間撹拌する。
有機相を55-65℃で水2.8リットルで洗浄し、続いて除去する。有機相から、4.2リットルを減圧下で蒸留して除く。続いて、メチルシクロヘキサン1.4リットルを65-75℃で添加し、その経過中に生成物が結晶化する。その懸濁液を15-25℃で8-16時間撹拌し、続いて0-5℃に冷却する。生成物を濾過により単離し、メチルシクロヘキサン4.2リットルで洗浄し、吸引乾燥し、35℃で減圧下で乾燥させる。
続いて乾燥粗物質(991g)を5倍量のメタノールとともに加熱、還流し、活性炭を添加し、その混合物を濾過する。メタノールを蒸留して除くことにより濾液を1.5リットルの容積に減少する。濾液を45-55℃に冷却した後、それをtert.-ブチルメチルエーテルで4倍の容積に希釈する。その懸濁液を0-5℃に冷却し、2時間撹拌し、吸引濾過し、tert.-ブチルメチルエーテルで洗浄し、真空乾燥キャビネット中で35℃で乾燥させる。
収量:899g(理論値の81.9%)
a.3-シアノ-2-(クロロメチル)-ピリジン
2-ヒドロキシメチル-3-ピリジンカルボキサミド165.5g(0.98モル)をオキシ塩化リン270mlと一緒に1時間にわたって90-100℃に加熱する。その反応混合物を室温に冷却し、続いて50-60℃で水約800mlに滴下して添加する。オキシ塩化リンを加水分解した後、その混合物を冷却しながら水酸化ナトリウム溶液で中和し、その経過中に生成物が沈殿する。それを濾過し、水300mlで洗浄し、続いて35-40℃で乾燥させる。
収量:122.6g(理論値の82%)
工程aの別法:3-シアノ-2-(クロロメチル)ピリジン
2-ヒドロキシメチル-3-ピリジンカルボキサミド20.0g(131.45ミリモル)をアセトニトリル110ml中で懸濁させ、78℃に加熱する。15分以内に、オキシ塩化リン60.65g(395.52ミリモル)を計量して入れ、その混合物を2時間にわたって81℃に加熱する。22℃に冷却した後、その反応混合物を40℃で水200ml中で撹拌する。トルエン100mlを添加した後、その混合物を冷却しながら水酸化ナトリウム溶液で中和する。相分離後に、有機相を水100mlで洗浄する。有機相を除去し、溶媒を減圧下で蒸発させて最初に油状残渣を生じ、これは放置すると結晶化する。
収量:16.66g(理論値の83%)
b.1-〔(3-シアノピリジン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-ブロモキサンチン
収量:257.5g(理論値の91%)
c.1-〔(3-シアノピリジン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-フタルイミドピペリジン-1-イル)-キサンチン
続いてこうして得られた粗生成物を沸騰メタノール1リットル中で撹拌し、熱時濾過し、メタノール200mlで洗浄し、続いて不活性下で70℃で乾燥させる。
収量:275g(理論値の88%)
d.1-〔(3-シアノピリジン-2-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノピペリジン-1-イル)-キサンチン
収量:273g(理論値の86%)
融点:188±3℃
実施例2及び3と同様にして、1-〔(3-メチルイソキノリン-1-イル)メチル〕-3-メチル-7-(2-ブチン-1-イル)-8-((R)-3-アミノピペリジン-1-イル)-キサンチンをまた調製する。
Claims (7)
- 下記の合成工程:
a)好適な溶媒中のrac-3-アミノピペリジンと無水フタル酸の反応及び
b)D-酒石酸の添加及び沈殿した酒石酸塩の単離によるこうして得られたラセミの3-(フタルイミド)ピペリジンの溶液からの(R)-3-(フタルイミド)ピペリジンの除去
を特徴とする、(R)-3-(フタルイミド)ピペリジンの調製方法。 - 下記の合成工程:
a)好適な溶媒中のrac-3-アミノピペリジンと無水フタル酸の反応及び
b)L-酒石酸の添加及び沈殿した酒石酸塩の単離によるこうして得られたラセミの3-(フタルイミド)ピペリジンの溶液からの(S)-3-(フタルイミド)ピペリジンの除去
を特徴とする、(S)-3-(フタルイミド)ピペリジンの調製方法。 - 下記の合成工程:
a)好適な溶媒中のrac-3-アミノピペリジンと無水フタル酸の反応及び
b)D-酒石酸の添加及び沈殿した酒石酸塩の単離によるこうして得られたラセミの3-(フタルイミド)ピペリジンの溶液からの(R)-3-(フタルイミド)ピペリジンの除去並びに
c)最初の塩沈殿のこうして得られた母液へのL-酒石酸の添加及び沈殿した(S)-3-(フタルイミド)ピペリジン酒石酸塩の単離
を特徴とする、(S)-3-(フタルイミド)ピペリジンの調製方法。 - 工程b)で使用される溶媒がエタノールである、請求項1から3の1項記載の方法。
- 鏡像異性的に純粋な8-(3-(R)-アミノピペリジン-1-イル)キサンチンを製造するための、請求項1記載の方法に従って調製された(R)-3-(フタルイミド)ピペリジン又はそのD-(-)-酒石酸塩の使用。
- 鏡像異性的に純粋な8-(3-(S)-アミノピペリジン-1-イル)キサンチンを製造するための、請求項2又は3記載の方法に従って調製された(S)-3-(フタルイミド)ピペリジン又はそのL-(+)-酒石酸塩の使用。
- 工程b)で単離された粗(R)-3-(フタルイミド)ピペリジン D-(-)-酒石酸塩が、アセトン及び水の混合物から再結晶される、請求項1記載の方法。
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