CAS: 107819-90-9; 1,3-Di-Boc-2-Methylisothiourea

该化合物是一种受保护的异硫素衍生物,广泛用于有机合成,特别是在丙酸和乙酸化学中,其主要优点包括:由于三氧碳基(Boc)保护组保护反应性异丁基乙醇,防止不受欢迎的副作用,因此加强了稳定性.2点的甲基替代进一步提高了核生殖反应的选择性.该化合物是将硫尿亚功能引入复杂分子的多用途中间体,同时尽量减少分解风险.它与标准的脱腐蚀条件的兼容性使其适合多步骤合成途径.双氧基保护还允许有控制的,连续的分离,以选择性功能化.

结构式图片

相似化合物

173998-77-1 215175-55-6 34840-23-8

欧盟法规

C&L通报

上下游产品

tert-butyl dicarbonatedi-tert-butyl dicarbonate S-Methylisothiourea sulfate carbamimidothioic acid methyl ester S-methylisothiourea hemisulphate ω,ω'(B°C)2-OHZ-Argω,ω'(B°C)2-OH tert-butyl (NE)-N-[amino-(tert-butoxycarbonylamino)methylene]carbamate methyl 4-(N-acetylamino)-5-[N',N-di(tert-butoxycarbonyl)guanidino]-3-(2-pentyloxy)benzoate

合成工艺路线路线简述

  • 合成目标产物 1,3-Di-Boc-2-Methylisothiourea 主要起始原料 Di-Tert-Butyl Dicarbonate And 2-Methyl-2-Thiopseudourea Sulfate
  • (文献来源)合成步骤主要原料 Di-Tert-Butyl Dicarbonate 和 2-Methyl-2-Thiopseudourea Sulfate

专利信息


专利号:US-2006264608-A1
优先权日:2001-08-03
标题 :Bi-directional synthesis of oligoguanidine transport agents
发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C
摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.

专利号:WO-2008105759-A1
优先权日:2007-02-27
标 题:Methods for synthesis of modified peptides
发明人:BROWER JUSTIN O
权利人:ARGOLYN BIOSCIENCE INC; BROWER JUSTIN O
摘要:Methods for the synthesis of peptides and peptide analogs containing aminoacid residues bearing substituted amino- and guanido- sidechains, such as alkyl lysine and arginine residues, are provided.

专利号:US-2023272006-A1
优先权日:2021-08-31
标题:Peptidomimetics and method of synthesis thereof
发明人:NEFZI ADEL
权利人:NEFZI ADEL; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES
摘要:The subject invention provides compounds, peptidomimetics, and methods of synthesis thereof. The subject invention provides the synthesis and use of guanidino acids and/or poly guanidino acids not only as vehicles for drug delivery but as toolbox for drug discovery. The peptidomimetic of the subject invention comprises oligo(guanidino acid)s or poly(guanidino acid)s with guanidines as peptide bond surrogates. The incorporation of the guanidine as amide bond surrogates offers significant differences in polarity, hydrogen bonding capability, and acid-base character.

专利号:WO-9943409-A1
优先权日:1998-02-27
标 题:Hplc fractionation of complex chemical mixtures
发明人:COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN
权利人:ISIS PHARMACEUTICALS INC; COOK PHILLIP DAN; CUMMINS LENDELL L; GRIFFEY RICHARD H; KAWASAKI ANDREW M; GAUS HANS; AN HAOYUN
摘要:The rapid deconvolution of complex chemical mixtures, such as combinatorial libraries prepared via solution-phase simultaneous addition of functionalities is demonstrated using HPLC. Libraries containing 25-216 members were screened for biological activity and active libraries are fractionated into discreet pools using preferred reversed-phase HPLC. The entire process can be completed from a single synthesis of 15-50 mg, without the need for fixed positions, serial synthesis, or tagging.

专利号:US-9359327-B2
优先权日:2008-06-30
标题:Process for the preparation of substituted pyrimidine derivatives
发明人:CESCO-CANCIAN SERGIO; CHEN HONGFENG; GRIMM JEFFREY S; MANI NEELAKANDHA S; MAPES CHRISTOPHER M; PALMER DAVID C; PIPPEL DANIEL J; SORGI KIRK L; XIAO TONG
权利人:JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to processes for the preparation of substituted pyrimidine derivatives, useful as intermediates in the synthesis of histamine H 4 receptor modulators, and to intermediates in H4 modulator synthesis.

专利号:US-11634741-B2
优先权日:2013-11-20
标 题:Synthesis of L-nucleic acids by means of an enzyme
发明人:PECH ANDREAS; JAROSCH FLORIAN; JAHNZ MICHAEL; KLUSSMANN SVEN; DAVID RALF
权利人:APTARION BIOTECH AG
摘要:The present invention is related to a method for adding one or more L-nucleotides to the 3′end of a first L-nucleic acid, wherein the method comprises the step of reacting the one or more L-nucleotides with the first L-nucleic acid in the presence of a protein comprising a mutant enzymatic activity exhibiting moiety, wherein the enzymatic activity is capable of adding one or more L-nucleotides to the 3′ end of the first L-nucleic acid, wherein the mutant enzymatic activity exhibiting moiety comprises an amino acid sequence, wherein the amino acids of the amino acid sequence are D-amino acids, wherein the mutant enzymatic activity exhibiting moiety is a variant of an enzymatic activity exhibiting moiety, wherein the enzymatic activity exhibiting moiety consists of an amino acid sequence according to SEQ ID NO: 15 and wherein the amino acids of the amino acid sequence according to SEQ ID NO: 15 are D-amino acids, wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety differs from the amino acid sequence of the enzymatic activity exhibiting moiety consisting of an amino acid sequence according to SEQ ID NO: 15 at least at one amino acid position, preferably at three amino acid positions, and/or wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety is a truncated form of an amino acid sequence according to SEQ ID NO: 15, and wherein the amino acid sequence of the mutant enzymatic activity exhibiting moiety is different from an amino acid sequence according to any of SEQ ID NOs 15 to 22 and 51.
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合成参考文献


摘要:Podlech, J., Science of Synthesis Knowledge Updates, (2019) 1, 406.
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