甲磺酸-2-丙炔-1-醇置于magnesium Bromide体系中,用 乙醚 用作溶剂,化学反应 1.0H,反应生成3-溴丙炔 参考文献:Synthése D'Alcools α-Alléniques Par Réaction D'Organochromiques Propargyliques Sur Les Aldéhydes Et Les Cétones 标题:Synthése D'Alcools α-Alléniques Par Réaction D'Organochromiques Propargyliques Sur Les Aldéhydes Et Les Cétones 摘要: Doi:10.1016/s0040-4020(01)92452-4
专利信息
专利号:US-6504041-B2 优先权日:1996-11-15 标题 :Synthesis of ruthenium or osmium metathesis catalysts 发明人:GRUBBS ROBERT H; BELDERRAIN TOMAS R; BROWN SETH N; WILHELM THOMAS E 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention relates to the synthesis of highly active ruthenium and osmium carbene metathesis catalyst in good yield from readily available starting materials. The catalysts that may be synthesized are of the general formula n wherein: n M is ruthenium or osmium; n X and X 1 are independently any anionic ligand; n L and L 1 are any neutral electron donor ligand; and, n R and R 1 are each hydrogen or one of the following substituent groups: C 2 -C 20 alkenyl, C 2 -C 20 alkynyl, C 1 -C 20 alkyl, aryl, C 1 -C 20 carboxylate, C 1 -C 20 alkoxy, C 2 -C 20 alkenyloxy, C 2 -C 20 alkynyloxy, aryloxy, C 2 -C 20 alkoxycarbonyl, C 1 -C 20 alkylthio, C 1 -C 20 alkylsulfonyl and C 1 -C 20 alkylsulfinyl. Optionally, the substituent group may be substituted with one or more groups selected from C 1 -C 5 alkyl, halogen, C 1 -C 5 alkoxy, and aryl. When the substitute aryl group is phenyl, it may be further substituted with one or more groups selected from a halogen, a C 1 -C 5 alkyl, or a C 1 -C 5 alkoxy. Specific synthetic protocols for vinyl alkylidene catalysts wherein R is hydrogen and R 1 is —CHCR 12 R 13 and non-vinyl alkylidene catalysts are also disclosed. In addition to the ease of synthesis (typically a one-step synthesis), the reactions generally may be run at or above room temperature and the resulting products usually may be used without extensive post synthesis purification.
专利号:US-11427596-B2 优先权日:2019-07-19 标 题:Metal-free solvent-free synthesis of fused-pyrido heterocycles and biomedical applications 发明人:CHELVAM VENKATESH; DUDHE PREMANSH; KRISHNAN MENA ASHA; SONAWANE AVINASH 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Embodiments herein provide fused-pyrido heterocycles such as azaindoles, carboline derivatives, furo[b]pyridines or furo[b]pyridine-isatin hybrids of Formula I.Embodiments also relate to a process for a synthesis of variety of complex pyrido-heterocycles The pyrido-heterocycles can be used for treating cancer (cervix, kidney, lung, breast and epidermal skin) and multi-drug resistant tuberculosis. These heterocycles can also be used as anti-biofilm agents against pathogenic strains, which will minimize the risk of secondary infections.
专利号:US-11945838-B2 优先权日:2018-12-20 标 题:Method for synthesis of protein amphiphiles 发明人:BRITTO Sandanaraj Selvaraj; REDDY Mullapudi Mohan 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES 摘要:The present invention discloses a novel cost effective method for synthesis of protein/peptide amphiphiles irrespective of functional and structural classification of proteins useful in designing a vaccine candidate from antigenic protein. The protein modification of the present invention is universal and hence any protein/peptide can be converted into amphiphilic proteins/peptides.
专利号:US-6376676-B1 优先权日:1993-06-30 标题 :Intermediates in the synthesis of (±)-camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; LIU HUI 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of novel intermediates in the synthesis of (±)-camptothecin and related compounds. The present synthesis scheme includes a novel 4+1 radical annulation followed by another cyclization to simultaneously assemble rings B and C of the camptothecin compound. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-6252079-B1 优先权日:1993-06-30 标 题 :Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; BOM DAVID 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursoris reacted with an aryl isonitrile having the formulawherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, agroup wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-8901352-B2 优先权日:2011-01-13 标题 :Method for the synthesis of rasagiline 发明人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN 权利人:REIS ÖMER; KOYUNCU HASAN; ESIRINGU ILKER; SAHIN YASEMIN; GULCAN H OZAN; NOBEL ILAÇ SANAYII VE TICARET A S 摘要:We have developed a new method for the synthesis of Rasagiline (Formula 1) based on the alkylation of trifluoroacetyl protected aminoindan. This protection enabled us to carry out an alkylation of aminoindan with a high yield and purity under very mild conditions with a wide range of reaction conditions and reagent selection. Considering the ease, purity and high yields of introducing and removal of the trifluoroacetyl group, this approach is a highly practical and economical way for the synthesis of rasagiline or its pharmaceutically acceptable salts.
参考文献:10.1007/s11010-011-0962-7 摘要:Świder R, Masłyk M, Martín-Santamaría S, Ramos A, de Pascual-Teresa B. Multisite-directed inhibitors of protein kinase CK2: new challenges. Molecular and Cellular Biochemistry. 2011 Jul 13;356(1-2):117. doi: 10.1007/s11010-011-0962-7. 参考文献:10.1107/s1600536811012578 摘要:Ouzidan Y, Kandri Rodi Y, Jasinski JP, Butcher RJ, Golen JA, El Ammari L. 1,3-Bis(prop-2-ynyl)-1H-1,3-benzimidazol-2(3H)-one. Acta Crystallogr E Struct Rep Online. 2011 Apr 13;67(5):o1091. doi: 10.1107/s1600536811012578. 参考文献:10.1107/s1600536811016862 摘要:Singh MK, Agarwal A, Mahawar C, Awasthi SK. tert-Butyl N-{2-[bis-(prop-2-yn-1-yl)amino]-phen-yl}carbamate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1382. 参考文献:10.1155/2011/854952 摘要:Ramapanicker R, Gupta R, Megha R, Chandrasekaran S. Applications of Propargyl Esters of Amino Acids in Solution-Phase Peptide Synthesis. International Journal of Peptides. 2011 Jun 16;2011():1–10. doi: 10.1155/2011/854952. 参考文献:10.1080/15257770.2011.582850 摘要:Moustafa AH, El-Sayed HA, Haikal Ael-F, El Ashry el SH. Synthesis of acyclovir and HBG analogues having nicotinonitrile and its 2-methyloxy 1,2,3-triazole. Nucleosides Nucleotides Nucleic Acids. 2011 May;30(5):340–52. doi: 10.1080/15257770.2011.582850.