CAS: 210992-28-2; 3-Amino-5-Fluorobenzonitrile

上下游产品

CAS号110882-60-5 3-氟-5-硝基苯腈 | CAS号64248-63-1 3,5-二氟苯甲腈 | CAS号557-21-1 氰化锌 | CAS号134168-97-1 3-氟-5-溴苯胺 | CAS号3819-88-3 1-氟-3-碘-5-硝基苯 | CAS号1435-51-4 1,3-二溴-5-氟苯 | CAS号807620-95-7 N-(3-bromo-5-fl... | CAS号723294-75-5 3-氟-5-碘苯甲腈 | CAS号507269-27-4 3-氟-5-[5-(吡啶-2-...

N-(3-Bromo-5-Fluorophenyl)Acetamide置于1,1'-双(二苯基膦)二茂铁,Sodium Hydroxide,Tris-(Dibenzylideneacetone)Dipalladium(0)体系中,用 N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 18.0H,反应生成5-氨基-3-氟苯腈
参考文献:3-[取代的]-5-(5-吡啶-2-基-2H-四唑-2-基)苄腈:鉴定高效和选择性的代谢型谷氨酸亚型5受体拮抗剂.
标题:3-[取代的]-5-(5-吡啶-2-基-2H-四唑-2-基)苄腈:鉴定高效和选择性的代谢型谷氨酸亚型5受体拮抗剂.
摘要:对3-(5-吡啶-2--2-基-2H-四唑-2-基)苄腈2的苯环的构效关系研究导致发现在3-位的小的非氢键供体取代基大大提高了体外效能.特别是3-氟-5-(5-吡啶-2-基-2H-四唑-2-基)苄腈(7)是一种高效且选择性的mglu5受体拮抗剂,具有非常好的大鼠药代动力学,脑渗透性和体内活性受体占用.
Doi:10.1016/j.Bmcl.2005.07.062

专利信息

专利号:US-6552018-B1
优先权日:1997-01-27
标 题:Pyrazole derivatives
发明人：EJIMA AKIO; OHSUKI SATORU; OHKI HITOSHI; NAITO HIROYUKI
权利人:DAIICHI SEIYAKU CO
摘要:The present invention relates to cis- and trans-forms of pyrazole derivatives, salts thereof, or agents containing the same, and represented by the general formula (I): n wherein G represents a nitrogen containing saturated heterocyclic structure represented by the following formula: n These compounds exhibit anti-tumor activity on 5-FU-resistant tumors and effects on P glycoprotein expressing, multiple-drug resistant tumors. An example of a pyrazole derivative which demonstrates 50% inhibition of tumor cell growth is 3-[4-(3-chloro-5-fluorophenyl)- 1 piperazinyl]-1-[1-(3-chloro-2-pyridyl)-5-methyl-4-pyrazolyl)-1-trans-propene hydrochloride. Synthesis of the compounds represented by formula (I) can be prepared by any one of various routes such as a Mannich reaction, a Wittig reaction, reductive amination or substitution by allylation.