스쿠알아민의 제조방법
    1.
    发明授权

    公开(公告)号:KR100255031B1

    公开(公告)日:2001-03-02

    申请号:KR1019980006425

    申请日:1998-02-27

    Abstract: PURPOSE: A process for producing squalamine is provided, thereby the squalamine can be cheaply and simply produced due to the use of cheap 3-keto-bisnocholenol as an initial compound. CONSTITUTION: The process for producing squalamine of formula(1) comprises the steps of: protecting a 3-keto group of 3-keto-bisnocholenol of formula(2) with an ethylenekital group and converting primary alcohol at C22 into an aldehyde group to produce 3-ethylenekital-23,24-bisnochola-5-en-22-al of formula(3); aldol condensing the compound of formula(3) to produce inone compound, hydrogenating the inone compound in the presence of platinum catalyst to produce 3-ethylenekital-cholest-5-en-24-on of formula(4); allyl oxidizing the compound of formula(4) to produce 3-ethylenekital-cholest-5-en-7,24-dion; selectively reducing double bond of the compound of formula(5) at C5 to produce 5alpha-cholestan and stereo selectively reducing a kito group at C7 and treating it with hydrochloric acid to produce 3-kito-5-alpha-cholestan-7,24-diol of formula(6); protecting hydroxy at C24 of the compound of formula(6) with t-butyldimethylsilyl, and converting kito at C3 to 3alpha-amino to produce 3alpha-amino-7,24-dihydroxycholest-5-en of formula(7); reacting the compound of formula(7) with polyamine aldehyde of formula(8) to produce a compound of formula(9); and treating the compound of formula(9) with acid to remove silly and a carbamate protecting group and to insert sulfone into the C24 site.

    한국형 중동호흡기증후군 코로나바이러스 감염에 감수성을 가지는 인간 DPP4 유전자를 전신에 발현하는 형질전환마우스와 이의 용도

    公开(公告)号:KR102207249B1

    公开(公告)日:2021-01-25

    申请号:KR1020200024827

    申请日:2020-02-28

    Abstract: 본발명은중동호흡기증후군코로나바이러스감염수용체인인간 Dipeptidyl peptidase 4 (human DPP4, hDPP4) 유전자를전신에발현하는형질전환마우스에관한것으로, 더욱상세하게는 CMV 프로모터; 인간 DPP4 유전자; 및 C 말단부위에 Flag 펩타이드를 tag시켜작동가능하게연결된인간 DPP4 유전자를발현하기위한재조합벡터로형질전환된, 인간 DPP4 유전자를발현하기위한형질전환마우스, 상기형질전환마우스를제조하는방법에관한것이다. 본발명의상기형질전환마우스는전신에 hDPP4 유전자발현을확인하였고, 한국형및 유럽형중동호흡기증후군코로나바이러스의특이적감수성을확인하였다. 중동호흡기증후군코로나바이러스가감염된 hDPP4 형질전환마우스는감염말기에모두급격한체중저하와더불어치사가일어났고, 심각한폐 손상이관찰되었다. 또한, 중동호흡기증후군코로나바이러스가감염된 hDPP4 형질전환마우스에서다양한염증성사이토카인분비가급격히일어남을확인하였다. 본발명에따른 hDPP4 전신발현형질전환마우스는중동호흡기증후군코로나바이러스감염성질병발달을규명하기위한 in vivo 연구에중요한동물모델로활용가능하며, 중동호흡기증후군코로나바이러스를제어하기위한백신및 치료제개발에매우유용하게활용가능하다.

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