专利号:US-7301006-B2 优先权日:2002-07-16 标 题 :Methods and materials for the synthesis of modified peptides 发明人:YOUNG TRAVIS G; KIESSLING LAURA L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Methods and protected amino acids useful as building blocks (protected monomers) for the synthesis of peptides and proteins that are selectively modified at one or more side-chain hydroxyl groups. Azide-bearing protecting groups allow the selective deprotection of side-chain hydroxyl groups of amino acids after synthesis of a peptide. Reaction conditions for removal of the azide-bearing protecting group can be selected which are substantially orthogonal to those that will remove α-amino protecting groups typically employed in peptide synthesis, such that hydroxyl groups protected with the azide-bearing protecting group remain protected during synthesis of the peptide chain. Various protecting groups which are readily available can be used for protecting potentially reactive side chain groups of amino acids in the peptide or protein to be modified. Preferred side-chain protecting groups are chemically distinguishable from the azide-bearing protecting group and substantially orthogonal reaction conditions can be selected such that side-chain protection of other amino acids is maintained when the azide-bearing protecting group is removed. The use of the azide-bearing protecting group of this invention for one or more hydroxy amino acids during peptide synthesis allows the selective unmasking of those azide-protected side-chain hydroxyl groups and selective modification of the hydroxyl groups that are selectively unmasked. The methods and materials herein are particularly used in synthesis of sulfated, phosphorylated and glycosylated peptides and proteins. Kits and methods of synthesizing a modified peptide or protein using the kits are also provided.
专利号:US-7939679-B2 优先权日:2006-01-19 标题:Method for synthesis of ciguatoxin CTX1B and compounds useful for the synthesis of ciguatoxin CTX1B 发明人:HIRAMA MASAHIRO; INOUE MASAYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Disclosed is a method for total synthesis of CTX1B, which is developed for the synthesis of a ciguatoxin analogue such as CTX3C and enables the more efficient application of an established reaction to the total synthesis of CTC1B. More specifically, disclosed is a method for total synthesis of CTX1B comprising; an O.S-acetal formation for synthesizing a novel compound (3); a radical cyclization reaction for constructing a 9-membered ring formation reaction including a novel compound (6) through a novel compound (8) and yielding a compound (D); and a deprotection for yielding CTX1B. Also disclosed are novel compounds (1) to (8) which are particularly useful for synthesis of CTX1B and can be used for the synthesis of a ciguatoxin analogue.
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-2007287843-A1 优先权日:2004-04-07 标题 :Methods and Intermediates for the Synthesis of Delta-9 Tetrahydrocannabinol 发明人:CABAJ JOHN E; PARIZA RICHARD J; LUKESH JULIE M 权利人:CABAJ JOHN E; PARIZA RICHARD J; LUKESH JULIE M 摘要:Processes are disclosed for the synthesis of Delta-9 tetrahydrocannabinol which result in an improved Y-THC/Y-THC ratio, and intermediates are disclosed that may be used in the synthesis of Delta-9 tetrahydrocannabinol such that improved Y-THCIY-THC ratios are achieved. The intermediates may be cyclic compounds prepared from 2-Carene. There is also provided a scaleable process for the preparation of (+)-p-menth-2-ene-1,8-diol, another intermediate used in the synthesis of delta-9-tetrahydrocannibinol.
专利号:US-6552213-B1 优先权日:2002-05-10 标 题:Stereoselective route to produce tris-O-substituted-(E)-1-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)ethene, an intermediate in the synthesis of trans-resveratrol 发明人:DESHPANDE PANDURANG BALWANT; SENTHILKUMAR UDAYAMPALAYAM PAL; ANDREW GNANAPRAKASAM 权利人:ORCHID CHEMICALS & PHARM LTD 摘要:The present invention relates to a new stereoselective method for the preparation of tris-O-substituted-(E)-1-(3,5-dihydroxyphenyl)-2-(4-hydroxyphenyl)ethene derivative of the formula (I) which is a key intermediate in the synthesis of trans-resveratrol (I, R2=R2=R3=H). The invention also provides a method for the exclusive synthesis of trans-isomer of compounds of formula (I) without any contamination of cis-isomer.
专利号:US-2024287126-A1 优先权日:2021-05-14 标 题:Novel synthesis of cholesterol 发明人:SCHINZER DIETER; SPIESS OLIVER; MUNT MAXIM; INDOLESE ADRIANO; ROUX LIONEL 权利人:CORDENPHARMA INT GMBH; UNIV OTTO VON GUERICKE MAGDEBURG; CORDENPHARMA INT 摘要:The invention relates to a synthesis of cholesterol; a ring opening step of the compound of formula (I) and subsequent activation and reduction step yielding cholesterol. The inventions relates also to intermediates achieved during said synthesis.
参考标题:Regioselective C-H Thioarylation Of Electron-Rich Arenes By Iron(III) Triflimide Catalysis 作者:Amy C. Dodds,Andrew Sutherland |发布日期:2021.4.16 摘要:Iron(III) Triflimide Allowed The Efficient Thiolation Of A Range Of Arenes, Including Anisoles, Phenols, Acetanilides, And N-Heterocycles. The Method Was Applicable For The Late-Stage Thiolation Of Tyrosine And Tryptophan Derivatives And Was Used As The Key Step For The Synthesis Of Pharmaceutically Relevant Biaryl Sulfur-Containing Compounds Such As The Antibiotic Dapsone And The Antidepressant Vortioxetine
合成参考文献
参考文献:10.1007/s00216-010-3471-8 摘要:Roeser J, Bischoff R, Bruins AP, Permentier HP. Oxidative protein labeling in mass-spectrometry-based proteomics. Analytical and Bioanalytical Chemistry. 2010 Feb 13;397(8):3441–55. doi: 10.1007/s00216-010-3471-8.