[미국특허]
Intermediates for the synthesis of oligonucleotide analogues
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
C07C-069/88
C07H-021/00
출원번호
US-0290587
(2002-11-08)
발명자
/ 주소
Cheruvallath, Zacharia S.
Ravikumar, Vasulinga T.
Cole, Douglas L.
출원인 / 주소
ISIS Pharmaceuticals, Inc.
대리인 / 주소
Woodcock Washburn LLP
인용정보
피인용 횟수 :
0인용 특허 :
20
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 independently H, alkyl, aryl, heteroaryl, alkaryl, or aralkyl; or R11and R12together with the carbon atoms to which they are attached form an optionally s
1. A compound having the formula: wherein: A is a diradical derived from a monocyclic or bicyclic aromatic ring system; R11and R12are each independently H, alkyl, aryl, 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; X1and X5are each independently O or S; X2is halogen; X3is --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; each R6is, independently, straight or branched chain alkyl having from 1 to 10 carbons; 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 or 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; and each R9is, independently, alkyl having 1 to about 10 carbon atoms, or aryl having 6 to about 10 carbon atoms. 2. The compound of claim 1, wherein A is phenylenyl with the moiety --OX4in the ortho or para position. 3. The compound of claim 1, wherein R11and R12are each H. 4. The compound of claim 1, wherein X1and X5are each O. 5. The compound of claim 1, wherein X2is chloro. 6. The compound of claim 1, wherein X3is --N(R6)2,where R6is isopropyl. 7. The compound of claim 1, wherein X4is benzoyl, acetyl or levulinyl.
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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