                         ˿µϣ20060530գ

06.05.30ûи
06.05.31, ӡĪСƶ򡱣
06.05.31, ԡѧнĹѧԺԺ˳ʮһйΡ
06.05.31, ѧԺ׾Ʒγ
06.05.31, R. ʷ˹ҽѧ
06.05.31, λ˼Լ˭Ȼλ˼
06.05.31, ̫ƽ֮ӡ帵Ԫڵ
06.05.31, ߸˹ɵĲ
06.05.31, һС㡶һ˿ǱˮԱĹܼ
06.05.31, ۿΡڡԭ̬ͨѧϮһ롰ߡȶ
06.05.31, СڡӺϿѧУ뿪ȥ
06.05.31, һסΪJACSļ
06.05.31, ʵ2ʮҵʵ֤Ϊ١
06.05.31, jizhengֹѧܵһ㽨顷
06.05.31, ҹлļײ¹һܾ־ֳ͵һ⹫
06.05.31, 21;ñ־һ
06.05.31, κ2006ȫ㲩ʿģҽѧݬ롷һ㲹
06.05.31, й걨û³Ѹ

˿(www.xys.org)(xys.dxiong.com)(xys.3322.org)(xys.xlogit.com)

                         ĪСƶ򡱣

                             ӡ

    Ǵڻͣÿ춼˵ĳֻӰ
ļΪһ˵ҲΪ
йءڶʮǰһ򱨵Ȼ󲨣
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    ǰո˹ȺĵоԱý͸¶˵
ǷһֻƶȺйءϢûʲô졣Ϊ
˵ƶɻµģⲢʵ뷨ϸͳŴѧ
սʱвŴѧҾôƹɴһּ
ӵȻԸġѧ˶ʹѧһʺ
ǽ塣

    һոŴѧƺڿ̸Ƿ֣
ƶȺУϸӵĺҪȸԣߵöࡣϸ
ʹϵͳھ״̬ʱ׼ϸ֡
ϸӵĺ߶ͯԼȻѡ
ĽƶȺԱȽϵĶ滷һӦԶͯ
ضԳȴкϵͳھ״̬ᵼ
֢շѪܵȼ˥ϡݳڸ˹綫
55꿴ȥ͸70һϣǵƽֻ64ꡣ

    оȥûʲôĵطоԱ
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ۣ˿ԽΪʲô˻Լƶʧȥ˸
Ȥ仰˵ƶѡĻֻ˰ƶֵ
ѹոý彫Ϊƶ򡱡

    ˵ĺһ˵ҲƶʹִҲ
Ƕ˵ƶǡŴġĻŵԣ
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۵ģҪصȺ໥ȽϲС

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ԲԡƶûֱӵĹϵҲƶ
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    ΪʷĻԭӢѧϲȥоƶ졣
1997꣬ӢѧҹһϷ޵ĺжӶ
ŮٷĺŮڶӡӢϷ޶෢
ϲ׼ٷ෢ĵײ㣬ƺ
ıҲƶ졣

    ʵѧͷˡȻѡԭһ
ȺŵȼͬȼĽ᲻ͬôԱҲ
ᷢ仯ȼϸߵģĶӣΪǵһӿԸ
Խ䣬죻ȼ͵ģŮ˶Ҳ
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    ﳤڽĲǵΪɱػϽ
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ʱҪء

2006.5.29

й걨2006.5.31.

(XYS20060531)

˿(www.xys.org)(xys.dxiong.com)(xys.3322.org)(xys.xlogit.com)

ѧнĹѧԺԺ˳ʮһй

ߣԣʵ

ʮһ1987񱱾ѧѧרҵʿѧλҵʦԴ
Ƽ͵ΪĹԱʽ϶Լعʹ
ģӴ˾ܾƼѧϽڼ䣬ʮһײһع
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ʮһڹְ˹Ī˹Los Alamosʵң
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ίĹҽܳ𡢹صĿ²Ǽƻȴ
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ʮһڱѧѧԺ ѧġݳʮһ漯ڲ
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http://202.200.112.9/jpk/apply/teacher/course_preview_index.jsp?curid=
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˿(www.xys.org)(xys.dxiong.com)(xys.3322.org)(xys.xlogit.com)

ҽѧ

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http://bmj.bmjjournals.com/talks/

ҪĻ⣺

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2. ҽѧעĿļٰ
3. ʲôǿף
4. ѧٵķĳ̶
5. ͻ
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1. ׵Σ

׾ŰͯǰǶԴȱʶ洦ɼҡ
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2. ҽѧעĿļٰ

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Ӣٰ

A. ڻT. ˵˹1990귢Ӣθѧ`ϵ
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һʡǣҽѧǷһֶԿ޶õĻͳ

3. ʲôǿף

Ϊ䶨˶ꡣŷһڽһ
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ڶ

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4. ѧٵķĳ̶

ԣȡѧٵĶ塣
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΢ؿ֮кιϵ

S. ĵо

ѯ80λԱˣӢˣҽѧ
ڡٷְٻشʡаϵ˵ٰ
ϵģɵĿгɹн6ƪı˻ش
ʱ֧ʣá١һʡ

ĵ֤ᣬ700ӢҽѧίԱᴦ30
ӢίԱᣨCOPEյ۹150

׵ķĳ̶

ظԼռȫĵ֮һ
ҽѧϵߴԼ֮һٲȫûво
ҽѧĵĴ漰ͻͻĹ5%

5. ͻԣ

6. ѧײԭ

ΪʲôᷢȫҲᷢ
ԭ֮һǱ뷢ĵѹ
ѵ㣬ûн̵еĴҵأʱ̵׵š
ǿԽѳͷΪƶεĻתġ

7. ӦԸף

ҽѧ缰쵼һҪ㹻ʶ
һȨе顢Ԥоһ⡣
ʲôٴɹʶ
پٱ˵ı
רŻٴ
ƶ
дҵصĹƶ
дҵصĽƶ

8. ίԱᣨCOPE

Ƕҽѧύĵ߳ŵĵֵǣ
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͡Ҷı༭ɡ

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ȷ֤ݵ80мƽƽܻ

У˵ظһͶ2918
15δ֪Ȩһͬ11Υµҽѧо11
δίԱͬ10

9. 

һ޷رܵ⡣δһܵӦԻ
һ⡣Ϊ˱⹫ڶҽѧоεıܵӦԻ
ҪġѧҲˣǣѧ磩жǻٻ
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λ˼Լ˭Ȼλ˼



120ҽѧĻѧ߹йѧĹ˼ҵۡ
۵ĽǶѧҪҪɵۼල۵һͨ
Natureļ߽ɵۼලйʷϵġĻᲢ
ۡһ˽Ƕʷ˿֪ǻնˣ
еһЩѾԵرֳƨɾԡǵص㡣 

ڲͬײŵǴϵĳͻվԼ
Լ汾Ȼġ෢ɡԼĻڽ̵ȵϲ㽨
ЭĳͻʹòͬײǵԺƽദᶯұ
ЭͻʧְʧܵĽ

ڲͬײǵ沩У⡰ʲ⡱ﵽ
⡱ʵ˫ӮǺƽǰ㹻ġ֪ͬʶɹʶ
Ч;֮һǲ˫Ļλ˼ʵУλ˼ҪռԴ
Ƶһȡʹ˫Ӯ˳

ռԴƵһǵûим̬ûΪ
һָľû㹻ţԽУе
ܵвʱͼԼλѹƶԷʶԽ
̬жġ𡱵̬˵ڲ
йִʷġNatureǰ˿ĸֱᲢֹۣ
ԴƵΪԼѧٱɣ
̬磨߱˶ĸȷ֪ĻΪ
ͼ˫ʶŬеһƬ԰ס

ΪʲôռԴƵһӦλ˼òʵڼΪ
ȣռԴƵһиʧ磬й
ȷٱߣɽġ¹гһͶġ˰ֹԱһ
ܱʧҵΡĿδڸλıٱ
ѡΣԴĸռ˵ĳɷ֣ӦĻм
ڵڶҲܶ˲ͬ⣬Լĳɹȫ鹦
˵ĴŬʵйдŬ˶úܣֻЩҡat 
right place, with right people, doing right thingsйѧѧ
ñȽϳɹ磬ѧеCASPEACGP programsв
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йѧһ벻ǰǸ̫ԭ족¼׷ѧΪ
ִҵܳߡǿѧҺ;ܹǫḳ
𾴺ȨʹãԾԾأ֮ı˽ǻǸ


ٻصЭ˵ǹ
˾ӡ塢ƶȵȣר
ǿʳƽǻ˼ǧڸײ沩ĵĲʹѵͳɹ
ĽᰲһҪԭһʵбβչ
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帵Ԫڵ

ߣ̫ƽ֮

Ԫ˵ˡ1ͬӢȻߵķ̸
س˺Ƿ׾ĽڡĻƤ2¶ڮ˿
άѧܵʵ

ǲԸԶⴧ˵ġġš
ʱǺõġԿ˸ǵĴBBCʱȻ
ǺõģΪԴǡǣˡȻ̸֮ҷ
֣Ķ⡣

ԪڶȺڴһֱġġͼĸܸ桱
ҥԡ3󣬸ԪڶȺڴ˲
ˡĸȺֱ͡ñӡ1Ȼĸ･
ԶȥǶκڰĪеͷȺ
ԶļСйͷʶĵĽ죬Ԫ
׳ܸ桱ҥԡֱһϵ˿ֲĸ
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Ԫû˵ĸȺֱ͡Щñ͸˭ġ
ǣйעѧٵ˶ܿóЩñҪ͵Ĳ͵İ
źͺſƽ̳ǶʩЧʥѧǷ
Ըŵ壬˿Ϊѧ
ٵҪؾ˿

ǲҪʸԪڣ˿ĸζģ˿ѧ
ʱˣ¶İҲٶˡԪڣøָָ
Щڡܸ桱˾ƽڣ̩˹˾ˣн
ѣλѣָָЩڸЩ
ɢҥԣЩдǴֱҪָôǿҪ˵
ܸ棬ɢҥԣдֱˡ

Ԫ˲ع˿˿ѵĲ
Ρȣ˿ѵĵ¡Уڵ˿Ѿǵ
ĺΪ˵ָǲεģġֱ˿
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ЩָǺ޸ݵ? Σ˿ѵʣΪֻרҺ
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ȫġ˿ҷĴ󲿷ְǳϮα죬ٵַǳԭʼ
ﷸϾרǵĴأһ棬ΪѶһЩС
Ȼ˿ȱרңԱκȫ¼˵Ϊط
˾ƽڡ緽нѺֿ֧طĺܶѲֳ൱̶ȵר
ҵ𣿸ԪڣҪǾǲˮ׼Сƣɷǵ


ԪԡȨʿԾӣԱΪΡǣκȫ
أκΪԺʿУѧ绤еίڵеطý
룬кͬԮܵĿƼͽȵ
ԺʿУ˵˿ǿأûǮҲûȨ
ҪйǯƣҪ⺣⻪˵Ĺûʹñߣ
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ʵԪڲظǸٳĹšרҵˮ׼͵λ
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ȨɲڵȨĿƼĳ֣ѡڮ
˿ġΪΪѡУǿ˸Ԫα

ǣȻдŵġλѧҡ˵˿
1䣬
˿乫ƽϽε̬ȣѾӮеġѧ
ӵ˿ڴˣȥ䵱ѧͥĽ
ɫͥϣָغͷָضжߵС
ʵαԼжϡ˿ҲǴš塱
ţάѧܹĸԪ־ġ

עͣ
1йָѧ٣˵ĸʽȺ David Cyranoski׫
壬ӢȻ2006524ա
2Ԫ˿ѺͶߵһ⹫š£ա
3Ԫ˿ѺͶߵһ⹫š£գ Ԫ
һۣƼߵĹţش˿ 513ա

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ɵĲ

߸˹

һЩѶҵķԵĻظȷǳлܹԵۣ
۵Ļֻнγɹͬ

ҵķûзɣʵһֱƳĶڹȥһֱ
ڣȷʵɲǱǱˡ

վ˵ûʲôĻҲǰ
Լ뷨˿漰ûκϵġ

νɣִѾķǳˣҮ۵ķɣ
Ҷ˵ɵĺǻȨȨĽޣΪһ˵
ɲҲûκνڽһ˵ĲɵĻϵġ

ͬҲˣʹԼɵͬʱҲزֹ
˵ɻ߶Ա˲˺

ȷڵǰй˵ɣɵĹ
չ˺ûиõİ취ýۼලȨ
ΪලҲҪһĻϣ仰˿Ƿ
ûκιϵ˿ѻܹж˿ǷһΪ
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֤ǱȻȫȷģкܶýʹලȨʱĺܲǡ

ʹ˿ûгֹκһԱ¶߲˺Ϊ
һķյģڹڵҲûа취İ취
Ч˿ܾͲôӰ

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޶˹ᵽᵽ⣬˼βȡ
ʩ֤һǺģ

ɵĿľΪ˽һֳ壬ǼҪý͸˵
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һ˵ʲôͦ˿ʲôģǷǴ˼ˣҵĸ˹۵
ǸйسĹ۵ûʲô⣬Ҳйѧල
ķ򣬶˿ҾǵȷпܴһЩ©ģͷ
˿֮Ļȫͬġ

ӭлл

2006.5.29

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    һ˿ǱˮԱĹܼ
    
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ܣӡˢƷǸٹ̵ģҪƭǼֱ̫ˡΪйũԺ
ооԱʿʦйԱйũҵѧԺܳ˲
ҪţֳǵĲƷ25ppmܹ
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ѧר˵ǵġʡܹ߶ٶ20~30%ֳ
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    ͦƭӵ˵ĳ֣ҳ˲ټʶҵľԹϣ
ˣƭƭˣȴͦҳƪۣáͷͷǵ
ʲô¶аԪΪʲôд120ţȥֻһܣ
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    ǰƵиĿǵúĽԱйѧĳ
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Աûشֻ˵Ҫõһ档ҿ
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    ʵѧҲãΡøҲգһ
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ءйڣ˷ӣҪٺܶġ

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ڡԭ̬ͨѧϮһ롰ߡȶ

ۿ

𾴵ķ

    ã˿ʵߡܾԼµҵտ
ߡ<ԭ̬ͨѧ>ϮһµĲͬ һģø
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    ǰϧѵġĴѧδƽֳϮ<
ԭ̬ͨѧ>Ϯһ·֡<ԭ̬
ͨѧ>Ϯһƪµϸ٣ԿĴѧѧ
ԺԺࡢ2003֮ԭ̬ͨѧ
һ鲿ȷϵϮˡѧۡһ顣ԴˣΪΪ࣬
ӦԸĳϮΪҪΣע⣺ǡҪΡȻ鼮Ϯ
ڵ׫дҲӦҪΣҪ۵⣩ѧ
ȨҲ֪һ㣬Ȿһѧļ/ڿ
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Ρļ/ѧڿȻʵ׫д˸ҪΣҲܶ
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Ϯַʵ׫дɴˡʵǵԭƶϮһҲӦ
𣬶ǻ͡ŵ߼Ϊ࣬ӦԼ
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ѵࣿķĿһ˰뿴
ⱾȨҳͼļɣ
http://www.duxiu.com/book/000/003/045/005/69211FA355B9D80F933AE2F2D2536ADD.htm

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ڡӺϿѧУ뿪ȥ



ʿ

˿΢ᣬƺֲ˵ǿλ
ĵѰʾβʿܲĳֹϵɡ

Ҵ1993굽2005һֱڻпƼѧϵ鹤ԭл
ѧԶƹϵԻ֪ܲˡᵽ
ˡȻѧҲҾһεѧɡǰУܼ
ڻеѧԺԿϵҵʦӿڣʿѧλӦ
ԿϵõġѧӵĶٻ֪ѧĿʦ廪
ͯʦרҵʦתϵѧѧԺ˽
ǣβʿͻĳɹĤƬǯڲʿ¹
ԺͻصڣȻ뿵ʦһѧѧԺʦ
εȲʿµĤƬǯоڹӦûֵóƵģȻڲᳫ
˵״оӦڹȴⷽ湤о֮һ

βʿڵ¹огɹġغ˽첩ʿ
ǻ໨ʱעһβʿо
http://www.ibp.ac.cn/c/04/contents/03/xutao.htmlͬĻа¡
Erwin Neher1991ŵҽѧβʿNeher
ʵҴ¹ĲʿоġNeherڵԺ
һʱ䡣ǹҵ״ʱڻ޷Լ
ŵߣôƸŵߵѧӦҲǺܺõѡNeher
ھڷĤƬǯĹ׶ŵġѧ
Ϊβʿʤεġ

Ȼĵǹֵ֮óƵЩʲ
ôǻһҪƸɡȻѧҲ
һƫСѧʿѡǴѧʿ¹Ľ˵¹Ŀѧ
ְλͬһѧУ룬ԭΪ˱׷ֳ
Լڵоⷽò̫ࡣҲ֪
һƫСѧʿǲǾָĻѧҵѧǵĻ
Щӻѧƫ˾ֻܷ䵽人нȥˣ
˾üƵò˳ˡһҵȴӺũˣ
ǻغˣоʲôѧҴ

ںܲĹϵû֤Ҳû֤˽пЦ
ĻԿϵ֮ԷչȽϼѣΪѧУĻеѧԺ̫ǿˣ
ĵ϶أǱרҵԿϵרҵصѺܶǵĻ
ᶼȥˡȻһЦѣѧϵԭԼɴ˰ʾ
һǣԿϵʦеѧԺʦʱߵòǺܽ
ǽƶϵνͲף
ﻯѧĳɹӦ߱ѡΪʸܲͬһ
ѧУҵԭѡΪĻҵ֮ܲڻ
߻غˡĻ޷ǰУĹϵ

ĵ濴λûûּڹڵ
µĸԣ󵨵Ĳ²һѣβʿʲô
·ˡ

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ΪJACSļ

һ

ϺлΪJACSϵļϣΪΪĵ
۷ôĿŵ٣ôͲ±ţ

1

Ĳ˵ˣλԲС㣨ʮ£õĸݣһ¡

Kaitocephalin: A mixture of 12 (74 mg, 0.1 mmol), 10 mg of 10% 
Pd/C and 5 mL of anhydrous methanol was stirred under hydrogen 
atmosphere (1 atm) for 30 min. After Pd/C was filtered off, the 
filtrate was concentrated. 

ΪֹӦĵһѾΪû˵ᴿ
ֲҲ֪Scheme 3ıע˵˸÷ӦĲ
Ϊ100

The residue was dissolved in 2 mL of methanol before 0.5 mL of 2 N 
HCl was added. The resultant solution was stirred for 1 h and then it 
was partitioned between ethyl acetate and saturated NaHCO3. The 
organic layer was separated and the aqueous layer was extracted with 
ethyl acetate. The combined organic layers was washed with water, and 
concentrated to give the crude amine. 

ΪֹӦĵڶѾΪû˵ᴿ
ֲػǲ֪Scheme 3ıע˵һĲ
Ҳ100

ȻЩСסڲϽķ롣ƻÿJACS
Ϊô˵ģ

Finally, 12 was transformed into kaitocephalin by following 
deprotection steps: (1) hydrogenolysis to remove benzyl group, (2) 
treatment with 2N HCl to remove Boc group and (3) hydrolysis with 1N 
NaOH to cleave the ester and oxazolidinone ring.

ֱΪǸûʵ飡Ǹ
12ȥBoc֮󣬵õһᡣô
ȡ԰С㵹ǿè壬ǣͼڸè壬˵ʲôȥ
BocͬʱҲǸȻˣԲȡⲻ
֪Ǳ׼ĲǽǽıС֪λС1N
ˮҺ4ļ״һСʱ֮ھʵ100ˣ
ΪΪλ˵÷ӦֻȥBocҲ˵Ϊ˵ǵġʵ顱
ֻȥBocûмԣԲСӦȴݸǡ

Ϊ˸÷ӻһȻԾͺͿȥ
ȡˡ漣ͳǲȡɹˣһ100ȡˣ
а

This amine was dissolved in 1 mL of methanol and 1 mL of THF. To 
this solution was added 0.5 mL of 1 N NaOH. The resultant mixture was 
stirred at 40 oC for 18 h. The cooled solution was adjusted pH to 7.0 
and then concentrated. The residue was purified by Dowex-50W using 
water as eluent to afford 45.1 mg (92%) of kaitocephalin.

һҲ档Dowex-50Wȥ޻ӣȻܹ
purifyǵĲһҲܸɾԣпǰ޻
ȥͿǡˡ92Ĳ൱ģȻ
ġ⡣Ϊ˵һĲӦǸ11
֪ظģдؾΪһͬ־ǣΪڲ
ṩȴһƷݡԣȻѾʶ˴
õƷһôǸǲҲøŸһĲ
ǡأײĶô˵ǸǸ11Ļ̫
ˣĻԼҲӴ

2ͼ

Ϊ˵X⾧֧ĳЩмĽۣ
ûϣ

ΪṩĹֻвֻףûӦ̼ף

е8ǾСûͼסѵ˿ô

ҪǣΪ˵ǵղȻķȫһǣ
ûκص֧˵ȻһҲûУ̫ˡ
ƪµΪ˷Ͱ

3Ϊĺϳɲݵô£

Ϊͬ־ǲҵģΪձ˲ȻĽṹͬʱҲϳ
ǸṹķӣTet. Lett. 2002, 43, 857-860ֽб£

ձ˺ϳɵĴ500Mz , D2O

1.57(m, 1H), 2.05(m, 1H), 2.09-2.15(m, 2H), 2.31(dd, 1H, 
12.2-6.7Hz), 2.36(m, 1H), 3.61(m, 1H), 3.81(d, 1H, 4.3Hz), 4.30(d, 1H, 
4.3Hz), 4.33(dd, 9.2-5.5Hz), 7.62(s, 2H).

ΪϳɵĴ300Mz , D2O

1.59 (m, 1H), 2.00 (m, 1H), 2.04(m, 1H), 2.11(m, 1H), 2.26(ddd, 
13.6-5.8-1.8Hz, 1H), 2.40(ddd, 13.9-6.8-15.7Hz, 1H), 3.68(m, 1H), 
4.15(br s, 1H), 4.33(dd, 7.9-6.1Hz), 4.40(br s 1H) 7.61(s, 2H).

ձ˷Ȼ500Mz , D2O

1.61(m), 2.01(m), 2.06(m), 2.12(m), 2.28(ddd, 14-6-2Hz), 2.41(ddd, 
14.5-7-6Hz), 3.70 4.16(br s), 4.35(dd, 8-6Hz), 4.41(br s), 7.62(s, 2H).

ɴ˿ɼΪõĲݣӦձϳɵ
IDENTICALģȴ漣ǸȻסIDENTICALˡ
ǸdddżʽҲˣаѽȻձһ
Ϊͬ־ò 

Ϊͬ־ġ(correction) [JACS2002V124(23)6792]
д

Total Synthesis of Kaitocephalin, the First Naturally Occurring 
AMPA/KA Receptor Antagonist [J. Am. Chem. Soc. 2001, 123, 9706-7].

Page 9707, Scheme 3: The last step should give a mixture of 
(2R,3S,4R,7R,9S)- and (2S,3S,4R,7R,9S)-isomers in a ratio of about 1/1 
via the unexpected racemization.  The detailed mechanism will be 
disccused elsewhere.  The configuration of kaitocephalin was revised 
as the (2R,3S, 4R,7R,9S) form (Okue, M.; kobayashi, H.; Shin-ya K.; 
Furihara K.; Hayakawa, Y.; Seto H.; Watanabe, H.; Kitahara, T.  
Tetrahedron Lett. 2002, 43, 857-60).

ձƪΪȻģ֤Ǹ2λϵİ
ĳЩǿ칹ġʵеĴҰⲻΪΪͬ־
ṩʵôԣΪͬ־JACSԭ⡰ˣ

Ȼǧǣһʧߣʧ񲻸ࣿԣΪͬ
־ȻɵءˣǸdetailed mechanism¾Ѳˡ¿
ҪǸѾͷæУΪԲ£ǸѾͷо顣

4

ȻˣǾи⡣ǣлҪչ
飬Ϊͬ־ʲôõĶԲôݹʹĳˣͨѶ
ӦøҪΡǣйһչйң
ΪԣߣҪ˰
ҹлѧҪʶ;һȽ׵İ취ǣ˾Ӷߣ
ǸСʱ˿̣СصǶκͿ顣
ΨһҪǣΪҪл쵼ҪǸ۲С

ȻбۡΪҲɵ˳˻ȡɹ
ؾԣܾ鿴ԭʼ¼ȫ֮ߡֻҪͦһأǾǲǰ
ͷﴺˡ

Although the story is a fiction, it does not mean that it could 
not happen.  ȨǰΪͬ־ı绤ʰɡΪͬ־һҪͦס

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ʮҵʵ֤Ϊ

ʵ2 

5-31-2006

ϺлΪJACS(J. Am. Chem. Soc. 2001,123, 9706-9707.)
ٺJACS¸(J. Am. Chem. Soc.2002, 124,6792)ٵۣΪ
strong2˵Ĺ۵ȷġ

ΪJACS¿ϳkaitocephalin2λS-Ͱᡣһ
(R)-Garnerȩ룬֡ɴĺϳƣܵõȻ2λR-
͡ԣΪƺϳɵĻȻͬ(identical)ǲȷġ
ңѾΪȷȫϳ֤ԣΪΪJACS١

ΪJACS¸һӦԤ벻õ
1/1ǴҲ١Ϊstrong2͵÷ǳ

Kaitocephalin1λΪᣬ2λΪR-Ͱ3λΪS-ǻΪ
2״0.52N HCl1СʱȥBOCš1Сʱ1λں
ˮĽвܷӦкܶĺϳ֤˵strong2ʹʱ1
λᱣȷġ

ΪJACS±1NˮoxazolidinoneΪ92%
ΪJACSSupporting1״1THFΪҺ0.51N
40½18СʱˮoxazolidinoneԼˮ4λ9λǣ
ΪJACS¸һӦԤ벻õ1/1
ܷ١

˷Ӧ£2λİǳȶܲ1/1
ԶǿΪķӦ2N80·Ӧ3Сʱ5Сʱ
12Сʱȥˮ3-ǻ-2-ữoxazolidinone
2λİƱD.A. Evans and A. E. Weber, 
J. Am. Chem. Soc., 1986,108,6757-6761ҪҿԽһṩ
10ƪڵо֤ʵΪĴ

ΪJACSµĺϳɷӦΪԽϺJonesӦ
(CrO3/H2SO4)ǻΪᣬJonesӦǿˮĲ²ܽ
ΪᣬûˮĲ뽫ͣȩĽ׶Ρǿ
BOCȥ

ΪJACSµĹݿΪûɼʹ
Kaitocephalinĺϳɹ˴ĺ˴Źײ˵ʲô

1990ͽҩ˾ҩз3-ǻ-2-
໯ǹĻ֮һǷǳϤһ
Ŀǰ쵼Լоҡ

һشʮ¡Ϊٲʧ󡷡ͬʱʮ
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׵ĶࡣסǮܷӾҪ٣޶ĿоѶʹ
õĻܷӵ󣬺ֹ

ҽ飺

1оֻڿСĿǰѧУȡֲĿоѣ
쾭塣ӦֹǮơ֣ѧУĹ̾
ʧˡʹѧУûֱӵľ룬ͨѧУȼҲ
Ŀġһ˵ǸѧУһҲӦĿƺϸ

2ҪԿоѽơùӦõõѧУİ
⣬ֶͨδѧУ򰴷ɴ

3ЩԲЧĿгơҵҹͬ
ǮƹҵֻҪԼĿɹ䣬
ҵȤġҵĿʧԽҲײһЩ

שˡ

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ҹлļײ¹һܾ־ֳ͵һ⹫

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ֳܾ

һĻֹԱڻ첿Źû
ӳһҹлļײĿΪ˸õشٽҵ
˽һλȽʵ쵼ǻĻԱܶ
Ϊʵ£컷߳õشٽ񾭼á
Ŀɳչڿʼ˵⣺

1.걨շѡͳԶΪһֱδ
ͳһ

շ

շǻߡȻѾҪ֧ߡ
ľɲͳһһȫвԤ㣻
յ۷ҪרռãҪȾι ֮䲻ùҹ
ʵǻܹɲ´ȫ۷
Ѿ͵ò֤ȫ˾͵úȥȫֻ󲿷
ˣԻΪӾ͵ðշѹͷȴץ겻
ֹ쵼¿һġ

еĻ֧ӣԭмʹְܵĹؼţְ
𻹰ֳִŷáװ߼豸רж
ȾԴȣֻǸҵλְͨڶԻʶ
Ӧĸл־ƵĻлӣԭмվ
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ˣСͨһֻոʮǮ˵ͲҲû취
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ټ㻹ʹؽȽС͵øѹեѹեʲ
ôˮ۵ĶգһҲݣҰշɹ涨ץס
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Ҷ֪

ۺԭͳƳշݱȻͲʵ

걨

ν걨ÿҵй״ıҵ
ĸȾŷŨȵȣԤŷ
ÿŷȣҪڻ˽״ΪҵȻ
ɵȥŷ1000ˮ϶ϱ1001֣ܱ800־Ͳˡ
ΪŴҲӣΪʵʹв޶ôҵ
ͷˡڶҵշѵֿ϶ǻֳݣ
Դ걨ͳƳ걨ݱȻҲʵ

ۻͳ

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ȫŷΪ2549֣Ŀ꣨1800֣749֣
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ŵշѹԱֶȽϸߣӽʵȻԺͳ
ˡһǹָ꣬и޶޶˵صĻ
ûãԻܳҪnεѹʽϱ
֪ԻͳҲǲ׼ȷġ

ȻжѹΪʲôȫֻôأһͳ
ƲŲͬͳƾָȫúͺŷȻ
ʵЧǲųʵϱĿܡ

֮Ŀǰڲûһ׼Զֻ
ǿ鹤ȷ㲻ͬȻֶܾ롰һ
̫޷ɣʵһ¡ܾ˾Ƶ
03ͿʼһֱòӲ̯ÿȻҪ6000Ǯ˺ա

ٻصղ˵շѹɣ03ֵܾ֡·
շѹָˮʩˮѵĶշѣ
ȫưнͷǽˮģضֽˮ
ܳŷŶշѣ̫ˣշѹȫ
Աȫը˹ûܾôɳǵ顣ˮŨ
꣬ˮҵͿ⽻۷⻹⣬ˮŨȳ
۷ôأַֹܳˮȡˮ
Ѷˮˮֱӿ۳ģŷCOD1000100ˮȡˮ
һģǶԳˮĸǴͬģֲ
շѣӵҪ֪ڳй趼൱ҵˮ
йĺٺٵģշѣûĻôշ
03˽ȫŶ׷ܾⷽ⣬ܾЩû
İȻô˲£һ䲻վͲհɾʹˣ
ûˣ

2.ëëţֻܾ˵󻰣ûָϿԽ

ܾһ׮¾ǡһ˫ꡱȫһ
㣬ȫȫ١νһ˫ꡱǵ2000Ⱦŷ
ơҵҵȾŷţйܾ꣬־ܸɳ
ĻҪȫ뿪չڻȫգԼҲǴʱ
㻷ֶʼˣ겻񰡣еĹҵҵŷſ
𣿶˻ôշѣɷҡ

˵˵µİɣֺܾٴҪȾԴԶϵͳ裬05
·28ʵͿչˣһ˲ƵĹܾ
һʼûϵͳسָļֹҲȷ28Ҳ˵÷ǳ
ͳνȾԴԶϵͳҵķˮۿڰװԶ
ͨ߷ʽݴ䵽ֵķⱾ뷨Ƿǳõģ
ҪһǮҪ֪һ׷ˮCOD߼豸ټݴ
豸20򣬶߼豸ټݴ豸50򰡣28
һǮҵֿܾǵʵûУҵ˭Ǯ
ԼҴſڿأ۷Ѷϵͳװ𣿾㰲ܾҲû
ӦĹ취ҵ϶뷽跨ڻֱ͵ˮ
⵽Ҫ˽ʵǵÿ˵ֳ鿴йҵôùܵİ
Ͷôܾ滮ûУ˵ǿùշѣ
շܼ⵽ݸûáĿǰ
װˮ߼⻹ûȷķһ䣬йصķɷֻ˵صȾ
ԴӦðװ߼⣬ʵûκεĿɲԣִܾδ´صȾԴ
˾׼䡣

Ŀǰضһѷڸ߼⣬˽ڰֳ
ԻؿۣĶĻԱҵװþֳָ豸
϶ȥһˣ

˵˵̬칤ɣһֱܾôģ
ҵȾûܺãʲô̬ʱûٺԭ
ҵֳֵ;ֳ̣Ӧ̬칤רŵĲŸ𣬻
ָ˼ңָܾٲˣʵ
ֻ˵󻰣ʩʲôûУȥɣ涼һͷˮչ
廨ţڣܾʶʣڸִһٵ
æһԱˡ

ѭùһ仰оίĹֲҪ
ˣɵ°ɡ

гĿ꿼ˡǿȣ˵ǿͷԼԼ
϶߸ְܾ쵼͸ɣΪͬ־
ˡ

޽Ŀ졣ĿǰҹĽĿ״Ƿǻûвͨģ
ܾһץ̫׳ˣܶԱڿ⻷Է
ӹ൱ʵʶ׬ǮҲһֻ۱һֻֻۣ
̹ܺʵʹнĿͶȺѰգܾ
Ҳָ̫٣ձ鶼

3.Աȱܲ

Ϻ񻷱ôֻٲǹԱ󲿷ֶǡ
ٲֵĹԱִܿչշѹ֣
ְֵֻܡڵǹԱ̫ˣɵĻ̫ˣ־
Ӧǹƶ࣬תƣô򣬻϶
֪ܾǸӴĻʲôۿ˾£æȥˣ
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𣿻Ͽ·ַֽһЩʵѡ

ĻԱȱʲô̶أ˵ɣͳм
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ͷǴŷãŷõļеڲҵ̡ô
ܷܾҲһֱûָϡĳһλܾ쵼꽲ָеĹҵ
ҵҪ걨Ұֳԣôȥ

кö໰Ҫ˵ʵ̫ˣϰ˵һֱд賿2㣬뵽
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21;ñ־һ

ô

ԹϣиԵվȡ˿Ҿúա
RUMOR˿˵˿̫û֡

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ͳˡÿ15ƪµeasyԴBBSͺöˣټϷ롢תʲô
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ǻҪÿѧΡӦ𽥰Ѿŵơ롰̡
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κ2006ȫ㲩ʿģҽѧݬ롷һ㲹

xqy

Ҳ֪κʦô,!

15. ˰
ʦ
λϺͨѧ
ĿѪںϻĿ¡͹о
ķPubMed δ
Ӱӣ
ѧƣٴҽѧ

1Bai-Wei Gu, Jiong Hu, Lan Xu,et al .Feasibility and Clinical 
Significance of Real Time Quantitative Reverse Transcription 
Polymerase Chain Reaction (RT-PCR) Assay .The Hematology Journal 
Haematologica2001 2, 330C340

2Gu BW, Xiong H, Zhou Y et al.Variant-type PML-RARalpha fusion 
transcript in acute promyelocytic leukemia: Use of a cryptic coding 
sequence from intron 2 of the RARalpha gene and identification -of a 
new clinical subtype resistant to retinoic acid therapy. Proc Natl 
Acad Sci U S A 2002 May 28;99(11):7640-5

3B-W Gu, Q Wang, J-M Wang et al. Major form of NUP98/HOXC11 fusion 
in adult AML with t(11;12)(p15;q13)translocation exhibits aberrant 
trans-regulatory activity. Leukemia 2003 17, 1858C1864

4  Shen ZX, Shi ZZ, Fang J, Gu BW,et al. All-trans retinoic 
acid/As2O3 combination yields a high quality remission and survival in 
newly diagnosed acute promyelocytic leukemia. Proc Natl Acad Sci U S A. 
2004 Apr 13;101(15):5328-35

5Shi JY, Shi ZZ, Zhang SJ, Zhu YM, Gu BW, et al. Association between 
single nucleotide polymorphisms in deoxycytidine kinase and treatment 
response among acute myeloid leukaemia patients. Pharmacogenetics. 
2004 Nov;14(11):759-68.

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û³Ѹ

2006-05-31й걨
 
    

    żȻμһսĿ³Ѹ22ŮܾҲһ
ֱ÷ƽ˾ѧ򹤡ż衢Ӿ

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    ³Ѹ⻷̨֡壬ֻż𣺡
˵³ѸŮ㽾ػش𣺡ûҾǡǻ
ΪֹΪҶ˽³ѸûиĻ̸Ҳûиĸ


    4ǰרŴȥһ㽭ˣι³Ѹʾӣȥ³
Ѹݡι֮Уƺδ³ѸߵøЩ

    ѧԺܾѡһšйѧСѧ½
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