Process for the synthesis of oligomeric compounds
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07F-009/02
C07H-021/00
출원번호
US-0016465
(2001-12-11)
발명자
/ 주소
Cheruvallath, Zacharia S.
Ravikumar, Vasulinga T.
Cole, Douglas L.
출원인 / 주소
ISIS Pharmaceuticals, Inc.
대리인 / 주소
Woodcock Washburn LLP
인용정보
피인용 횟수 :
1인용 특허 :
19
초록
Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. Also provided are synthetic intermediates useful in such processes.
대표청구항▼
1. A compound having the formula: wherein A is a diradical derived from a monocyclic or bicyclic aromatic ring system; R11and R12are each H, independently alkyl, aryl, heteroalkyl, heteroaryl, alkaryl, or aralkyl; or R11and R12together with the carbon atoms to which they are attached form an
1. A compound having the formula: wherein A is a diradical derived from a monocyclic or bicyclic aromatic ring system; R11and R12are each H, independently alkyl, aryl, heteroalkyl, heteroaryl, alkaryl, or aralkyl; or R11and R12together with the carbon atoms to which they are attached form an optionally substituted aliphatic or aromatic ring having from 4 to 6 ring atoms; X4is alkaryl, aralkyl, sulfonyl, thiol, substituted sulfonyl, or substituted thiol, wherein said substituent is alkyl, aryl, or alkaryl; or X4is a group of formula --C(=O)--(O)aa--R40where aa is 0 or 1 and R40is lower alkyl, aryl, aralkyl, heteroaryl wherein said lower alkyl, aryl, aralkyl or heteroaryl groups are optionally substituted with one or more alkyl, aryl, aralkyl, halo or acetyl groups; or X4is a group of formula --(--CH2--CH2--)dSi(R9)3where d is 0 or 1; each R9is, independently, alkyl having 1 to about 10 carbon atoms, or aryl having 6 to about 10 carbon atoms; X1and X5are each independently O or S; R5is --N(R6)2,or a heterocycloalkyl or heterocycloalkenyl ring containing from 4 to 7 atoms, and having up to 3 heteroatoms selected from nitrogen, sulfur, and oxygen or optionally one of said R5groups is chloro; and R6is straight or branched chain alkyl having from 1 to 10 carbons. 2. The compound of claim 1 wherein A is phenylenyl with the moiety --OX4in the ortho or para position, or A is naphthalidenyl connected to X5at the 1-position, with the moiety --OX4being in the 5- or 6-position, and X1and X5are each O. 3. The compound of claim 2 wherein X4is benzoyl, acetyl, or levulinyl. 4. The compound of claim 3 wherein one of said R5groups is --N(R6)2where R6is isopropyl. 5. The compound of claim 4 wherein one of said R5groups is chloro.
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이 특허에 인용된 특허 (19)
Cook Phillip Dan ; Manoharan Muthiah ; Kawasaki Andrew Mamoru, 2'-O-aminooxy-modified oligonucleotides.
Andrus William A. (San Francisco CA) Efcavitch J. William (Belmont CA) McBride Lincoln J. (Redwood City CA), Chemical capping by phosphitylation during oligonucleotide synthesis.
Cook Phillip Dan ; Sanghvi Yogesh S. ; Sprankle Kelly G. ; Ross Bruce S. ; Griffey Rich H., Oligomeric compounds having pyrimidine nucleotide (S) with 2'and 5 substitutions.
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