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项目整合精选>>>Indium In 111 pentetreotide, 111In-Pentetreotide, 111In-DTPA-octreotide, MP-1727, DTPA-SMS(noncomplexed)
Indium In 111 pentetreotide, 111In-Pentetreotide, 111In-DTPA-octreotide, MP-1727, DTPA-SMS(noncomplexed)
喷曲肽 Chemical Name: Hydrogen [N-[2-[[2-[bis(carboxymethyl)amino]ethyl](carboxymethyl)amino]ethyl]-N-(carboxymethyl)glycyl-D-phenylalanyl-L-cysteinyl-L-phenylalanyl-D-tryptophyl-L-lysyl-L-threonyl-N1-[2(R)-hydroxy-1(R)-(hydroxymethyl)propyl]-L-cysteinamide cyclic (3--8)-disulfidato(4-)]indate(1-)-111In
CAS No. 139096-04-1, 138661-02-6 (non-complexed)
项目整合开发状态: Launched-1994
项目研究机构: Mallinckrodt (Originator), Novartis (Originator), Altana Pharma (Licensee)
合成路线:The selective protection of D-Phe1-octreotide peptide (I) with Boc2O gives the monoprotected peptide (II),which is condensed with diethylenetriaminopentaacetic acid (DTPA) dianhydride (III) by means of NaHCO3 in dioxane/water to yield the adduct (IV).The treatment of (IV) with TFA affords the desired DTPA-octreotide derivative (V),which is finally labeled with 111InCl3 in acetic acid or in ammonium citrate to afford the target indium derivative.The starting D-Phe1-octreotide peptide (I) has been obtained by the conventional methods of peptide synthesis using a peptide synthesizer.
📌 参考资料/链接：
参考文献标题:[111In-DTPA-D-Phe1]-octreotide,a potential radiopharmaceutical for imaging of somatostatin receptor-positive tumors: Synthesis,radiolabeling and in vitro validation
文献作者:Bakker,W.H.; Albert,R.; Bruns,C.; Breeman,W.A.; Hofland,L.J.; Marbach,P.; Pless,J.; Pralet,D.; Stolz,B.; Koper,J.W.; et al.
参考来源:Life Sci 1991,49(22),1583
📄 详细内容
合成路线:The selective protection of D-Phe1-octreotide peptide (I) with Boc2O gives the monoprotected peptide (II),which is condensed with diethylenetriaminopentaacetic acid (DTPA) dianhydride (III) by means of NaHCO3 in dioxane/water to yield the adduct (IV).The treatment of (IV) with TFA affords the desired DTPA-octreotide derivative (V),which is finally labeled with 111InCl3 in acetic acid or in ammonium citrate to afford the target indium derivative.The starting D-Phe1-octreotide peptide (I) has been obtained by the conventional methods of peptide synthesis using a peptide synthesizer.
参考文献标题:Generally applicable,convenient solid-phase synthesis and receptor affinities of octreotide analogs
文献作者:Edwards,W.B.; Fields,C.G.; Anderson,C.J.; Pajeau,T.S.; Welch,M.J.; Fields,G.B.
参考来源:J Med Chem 1994,37(22),3749
合成路线:The selective protection of D-Phe1-octreotide peptide (I) with Boc2O gives the monoprotected peptide (II),which is condensed with diethylenetriaminopentaacetic acid (DTPA) dianhydride (III) by means of NaHCO3 in dioxane/water to yield the adduct (IV).The treatment of (IV) with TFA affords the desired DTPA-octreotide derivative (V),which is finally labeled with 111InCl3 in acetic acid or in ammonium citrate to afford the target indium derivative.The starting D-Phe1-octreotide peptide (I) has been obtained by the conventional methods of peptide synthesis using a peptide synthesizer.
参考文献标题:Direct solid phase synthesis of biologically active peptide alcohols
文献作者:Wu,Y.-T.; et al.
参考来源:J Chin Chem Soc (Taipei) 1999,46(2),135
合成路线:The selective protection of D-Phe1-octreotide peptide (I) with Boc2O gives the monoprotected peptide (II),which is condensed with diethylenetriaminopentaacetic acid (DTPA) dianhydride (III) by means of NaHCO3 in dioxane/water to yield the adduct (IV).The treatment of (IV) with TFA affords the desired DTPA-octreotide derivative (V),which is finally labeled with 111InCl3 in acetic acid or in ammonium citrate to afford the target indium derivative.The starting D-Phe1-octreotide peptide (I) has been obtained by the conventional methods of peptide synthesis using a peptide synthesizer.
参考文献标题:Direct solid-phase synthesis of octreotide conjugates: Precursors for use as tumor-targeted radiopharmaceuticals
文献作者:Hsieh,H.P.; Wu,Y.T.; Chen,S.T.; Wang,K.T.
参考来源:Bioorg Med Chem 1999,7(9),1797
合成路线:The selective protection of D-Phe1-octreotide peptide (I) with Boc2O gives the monoprotected peptide (II),which is condensed with diethylenetriaminopentaacetic acid (DTPA) dianhydride (III) by means of NaHCO3 in dioxane/water to yield the adduct (IV).The treatment of (IV) with TFA affords the desired DTPA-octreotide derivative (V),which is finally labeled with 111InCl3 in acetic acid or in ammonium citrate to afford the target indium derivative.The starting D-Phe1-octreotide peptide (I) has been obtained by the conventional methods of peptide synthesis using a peptide synthesizer.
参考文献标题:Conventional and high-yield synthesis of DTPA-conjugated peptides: Application of a monoreactive DTPA to DTPA-D-Phe1-octreotide synthesis
文献作者:Arano,Y.; et al.
参考来源:Bioconjugate Chem 1997,8(3),442
产品链接: CAS No. 139096-04-1›› 产品链接: CAS No.138661-02-6››