CAS: 3930-83-4; 2-Iodobenzamide

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CAS号88-67-5 邻碘苯甲酸 | CAS号4387-36-4 2-碘氰基苯 | CAS号609-67-6 2-碘苯甲酰氯 | CAS号57-13-6 尿素 | CAS号118-92-3 邻氨基苯甲酸 | CAS号1885-29-6 2-氨基苯甲腈 | CAS号104919-72-4 ethyl N-(2-hex-... | CAS号109722-74-9 6,11-dihydroind... | CAS号4387-36-4 2-碘氰基苯 | CAS号360-64-5 2-(三氟甲基)苯甲酰胺 | CAS号1133467-89-6 [N-(trifluorome... | CAS号402-43-7 对溴三氟甲苯 | CAS号1769-24-0 2-甲基-4(1H)-喹唑啉酮 | CAS号18818-37-6 2-naphthalen-1-... | CAS号193882-91-6 (3-oxo-2H-1λ3,2... | CAS号1022-45-3 2-苯基-4-[3H]喹唑啉酮

2-碘苯甲醛置于甲酸,硝基甲烷,三氟甲磺酸酐体系中,用 溶剂黄146 用作溶剂,化学反应 12.0H,以60%的收率获得2-碘苯甲酰胺
参考文献:硝基甲烷作为施密特型酰胺和腈形成中的氮供体
标题:硝基甲烷作为施密特型酰胺和腈形成中的氮供体
摘要:从硝基甲烷中获取氮气 硝基甲烷大量生产用作溶剂.它作为试剂的应用主要集中在甲基质子在改变碳中心的过程中的酸度.刘等人.现在报告一种替代方案,该方案激活氮中心以产生胺化剂.与三氟甲磺酸酐,甲酸和乙酸的原位还原反应产生乙酰化羟胺,通过质谱法表征.这种氮供体可以方便地将各种酮和醛转化为酰胺.科学,这个问题 P.281 方便地从硝基甲烷原位衍生的乙酰化羟胺可以将酮和醛转化为酰胺.自 1923 年发现以来,施密特反应一直是酰胺和腈的有效且广泛使用的合成方法.然而,其应用通常需要使用挥发性,潜在爆炸性和剧毒的叠氮试剂.在这里,我们报告了一个序列,其中三氟甲磺酸酐和甲酸和乙酸激活大量化学硝基甲烷,作为氮供体代替类施密特反应中的叠氮化物.该协议进一步将底物范围扩展到炔烃和简单的烷基苯,用于制备酰胺和腈.我们报告了一个序列,其中三氟甲磺酸酐和甲酸和乙酸激活大量化学硝基甲烷,作为氮供体代替类施密特反应中的叠氮
Doi:10.1126/science.Aay9501

专利信息

专利号:WO-2025108921-A1
优先权日:2023-11-22
标 题 :Synthesis of radiopharmaceutical agents
发明人：AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL
权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER
摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.

专利号:US-8697032-B2
优先权日:2003-05-02
标题:Prosthetic groups attached to stannyl polymer in the synthesis of radiopharmaceuticals
发明人：HUNTER DUNCAN; GAGNON M KAREN J
权利人:UNIV WESTERN ONTARIO
摘要:The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds that can be converted to radiopharmaceutical compounds in one step. In a preferred embodiment, a radiopharmaceutical precursor is bound to a polymeric support via a prosthetic group comprising an alkenyl-tin bond. The radiopharmaceutical precursor is converted to a radiopharmaceutical compound in one step involving cleavage of the alkenyl-tin bond and incorporation of a radioisotope to form the radiopharmaceutical compound. Importantly, the polymeric support containing the toxic tin by-product can be easily removed from the radiopharmaceutical compound by filtration. The present invention can be used to install a large number of different radioisotopes. In a preferred embodiment, the radioisotope is 211 At, 123 I, or 131 I.

专利号:US-8231858-B2
优先权日:2003-02-10
标 题 :Diagnostic imaging agents with MMP inhibitory activity
发明人：STOREY ANTHONY; DAVIS JULIE; RICKETTS SALLY-ANN; MENDIZABAL MARIVI; CUTHBERTSON ALAN; ARUKWE JOSEPH; HEYWOOD KIRSTY; WILSON IAN; WYNN DUNCAN; SCHAFERS MICHAEL; LEVKAU BODO; WAGNER STEFAN; BREYHOLZ HANS-JOERG; KOPKA KLAUS
权利人:STOREY ANTHONY; DAVIS JULIE; RICKETTS SALLY-ANN; MENDIZABAL MARIVI; CUTHBERTSON ALAN; ARUKWE JOSEPH; HEYWOOD KIRSTY; WILSON IAN; WYNN DUNCAN; SCHAFERS MICHAEL; LEVKAU BODO; WAGNER STEFAN; BREYHOLZ HANS-JOERG; KOPKA KLAUS; GE HEALTHCARE LTD
摘要:The present invention relates to the field of diagnostic imaging. Specifically, the invention relates to the diagnostic imaging of diseases where specific matrix metalloproteinases are known to be involved. One embodiment of the invention is a compound having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the diagnostic imaging agent of the invention in a form suitable for mammalian administration. The invention furthermore discloses intermediates in the synthesis of the diagnostic imaging agents of the invention and kits for the preparation of the pharmaceutical composition of the invention. The pharmaceutical composition of the invention may be used in the diagnosis of diseases where specific matrix metalloproteinases are known to be involved.

专利号:WO-2024044825-A1
优先权日:2022-09-01
标 题:Compound collections, compounds and synthesis thereof
发明人：FLYNN BERNARD; CHEN SHUQI; PRIEBBENOW DANIEL; JASZEWSKI LEO
权利人:UNIV MONASH
摘要:Provided herein are collections of compounds of formula a) to u), and salts thereof, which have polycyclic aromatic scaffolds and thus have structures targeted towards binding polynucleotide therapeutic targets, including polynucleotide-protein complexes. Also provided are compounds and salts themselves, methods of synthesizing such compounds, methods of identifying compounds having activity against a polynucleotide target, use of the compounds as reference compounds in assays, and phenotypic methods of identifying a new polynucleotide target using the compounds.

专利号:EP-1624901-A2
优先权日:2003-05-02
标题 :Prosthetic groups attached to stannyl polymer in the synthesis of radiopharmaceuticals

专利号:JP-2009132713-A
优先权日:2007-11-30
标题:Improved catalytic synthesis of diaryl ethers