CAS: 772-79-2; 4-Chlorophenyl Phosphorodichloridate

上下游产品

CAS号106-48-9 对氯苯酚 | CAS号871896-25-2 4-dichlorophosp... | CAS号10026-13-8 五氯化磷 | CAS号98-67-9 对羟基苯磺酸 | CAS号18264-30-7 (4-chlorophenyl... | CAS号106-46-7 1,4-二氯苯 | CAS号113813-22-2 3-[(4-chlorophe... | CAS号69497-44-5 4-氯苯基磷酸铵氯化氯苯酯 | CAS号77181-80-7 4-CHLOROPHENYL-... | CAS号81366-72-5 4-CHLOROPHENYL-... | CAS号83416-83-5 (4-chlorophenyl... | CAS号52883-42-8 6-pyridin-1-ium... | CAS号62420-37-5 1-[(4-chlorophe... | CAS号62868-66-0 1-chloro-4-diam...

📜对氯苯酚置于三乙胺,三氯氧磷体系中,用 四氢呋喃,乙醚 作为反应溶剂,化学反应生成 4-氯苯基二氯磷酸酯
参考文献:氨基磷酸酯protide技术的应用显着提高了碳环腺苷衍生物的抗病毒效力.
标题:氨基磷酸酯protide技术的应用显着提高了碳环腺苷衍生物的抗病毒效力.
摘要:我们报告了氨基磷酸酯原核苷酸(protide)技术在抗病毒剂碳环l-D4A(l-Cd4A)中的应用.l-Cd4A的苯基甲基丙氨酸基母体protide是通过格利雅(grignard)介导的磷酰氯反应制备的,得到的化合物具有显着改善的抗hiv(2600倍)和hbv活性.我们描述了protide的芳基,酯和氨基酸区域的修饰,以及这些变化如何影响抗病毒活性和代谢稳定性.注意到针对hiv和hbv的sar分别且不同.另外,由d-核苷d-Cd4A和双脱氧类似物l-Cdda和d-Cdda制备protide.与母体药物相比,这些化合物显示出更适度的效能改善.综上所述,当将protide方法应用于l-Cd4A时,在体外的效价提高了9000倍,非常成功,抗hiv的能力提高了.为了临床前候选人的选择,我们使用食蟹猴肝脏和肠道s9馏分进行了代谢稳定性研究.
DOI:10.1021/jm060776W

专利信息

专利号:US-5204456-A
优先权日:1986-04-08
标题:Derivatives of nucleosides and their use for the synthesis of oligonucleotides
发明人：MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT
权利人:COMMISSARIAT ENERGIE ATOMIQUE
摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or a alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucelotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.

专利号:US-7595390-B2
优先权日:2003-04-28
标 题:Industrially scalable nucleoside synthesis
发明人：MOUSSA ADEL; WANG JING YANG; STORER RICHARD
权利人:NOVARTIS AG
摘要:An industrially scalable two-step process for preparing a β-L-2′-deoxy-nucleoside that results in a predominance of the β- over the α-anomeric form of the compound is described. An optional third step may be used to prepare 3′-prodrugs of desirable β-L-2′-deoxy-nucleosides for the delivery of these pharmaceuticals effective for treating viral diseases. The synthetic process is applicable in particular to the formation of β-L-2′-deoxy-cytidine, a pharmaceutically acceptable salt or prodrug thereof. The process can provide a relatively uncontaminated product that may require no further isolation or purification, thereby making the synthesis easily scalable for industrial manufacture.

专利号:EP-0155950-B1
优先权日:1983-09-02
标题 :Oligonucleotide polymeric support system
发明人：ARNOLD LYLE J JR
权利人:MOLECULAR BIOSYSTEMS INC
摘要:A versatile polymeric support system for the synthesis of oligonucleotides featuring a universal primer which allows chain elongation, in either the 3' or 5' direction, with any currently available DNA or RNA synthesis method, by a process which utilizes oxidatively cleaved primers to facilitate chain elongation and release. The support system is capable of withstanding mildly basic and acidic reaction conditions, while still permitting a convenient and quantitative release, either before or after removal of protecting groups from reactive groups, of synthesized oligonucleotides from a single polymeric support. Removal of the protecting groups before cleavage of the oligomer from the support permits the use of the immobilized oligomer as an affinity hybridization support for both isolation and detecting complementary polynucleic acids.

专利号:US-4980460-A
优先权日:1986-04-08
标 题 :Protected nucleosides which permit more efficient oligonucleotide syntheses
发明人：MOLKO DIDIER; SCHULHOF JEAN-CLAUDE; TEOULE ROBERT
权利人:COMMISSARIAT ENERGIE ATOMIQUE
摘要:The invention relates to derivatives of nucleosides and their use for the synthesis of oligonucleotides. These derivatives are in accordance with the formula: (I) in which B represents a radical derived from guanine, cytosine or adenine, whose exocylic NH group is protected by the group with R1 representing a hydrogen atom or an alkyl radical and R2 a hydrogen atom, and alkyl radical, an alkoxy radical and optionally substituted aryloxy radical, R3 represents a hydrogen atom, the dimethoxytrityl radical or the radical R4 represents a hydrogen atom, the radical of formula: or a radical suitable for the synthesis of polynucleotides and R5 represents a hydrogen atom or the protected or unprotected hydroxyl OH radical.

专利号:US-5539097-A
优先权日:1983-09-02
标题 :Oligonucleotide polymeric support system
发明人：ARNOLD LYLE J JR
权利人:MOLECULAR BIOSYSTEMS INC
摘要:A versatile polymeric support system for the synthesis of oligonucleotides is provided featuring a universal primer which allows chain elongation, in either the 3' or 5' direction, with any currently available DNA or RNA synthesis method, by a process which utilizes oxidatively cleaved primers to facilitate chain elongation and release. The support system is capable of withstanding mildly basic and acidic reaction conditions, while still permitting a convenient and quantitative release, either before or after removal of protecting groups from reactive groups, of synthesized oligonucleotides from a single polymeric support. Removal of the protecting groups before cleavage of the oligomer from the support permits the use of the immobilized oligomer as an affinity hybridization support for both isolating and detecting complementary polynucleic acids.

专利号:US-5362866-A
优先权日:1983-09-02
标 题:Oligonucleotide polymeric support system with an oxidation cleavable link
发明人：ARNOLD LYLE J JR
权利人:MOLECULAR BIOSYSTEMS INC
摘要:A versatile polymeric support system for the synthesis of oligonucleotides is provided featuring a universal primer which allows chain elongation, in either the 3' or 5' direction, with any currently available DNA or RNA synthesis method, by a process which utilizes oxidatively cleaved primers to facilitate chain elongation and release. The support system is capable of withstanding mildly basic and acidic reaction conditions, while still permitting a convenient and quantitative release, either before or after removal of protecting groups from reactive groups, of synthesized oligonucleotides from a single polymeric support. Removal of the protecting groups before cleavage of the oligomer from the support permits the use of the immobilized oligomer as an affinity hybridization support for both isolating and detecting complementary polynucleic acids.