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Synthetic cyclic peptides used as models for conformational analysis and as potential drugs
Synthetic cyclic peptides used as models for conformational analysis and as potential drugs
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机译：合成环肽用作构象分析模型和潜在药物
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摘要
Production of a cyclic tetrapeptide (I) comprises forming a cyclotetrapeptide complex (II) by reacting a dipeptide ester (IIIa) or a tetrapeptide ester (IIIb) with a transition metal salt or complex in the presence of a base, precipitating the complex with a compound containing a suitable cation, releasing (I) from the complex by reaction with a protonic acid, and isolating (I). Compounds used in the reactions have the formulas: Kat(x+zy)+ = Mx+(C(R)(CHR')mC(O)N-(C(R)(CHR')mC(O)N-)2C(R)(CHR')mC(O)N)y-z(x-zy)- (II) M = transition metal ion; R = H or organic groups optionally substituted by OH, amino, COOH and/or amide groups; R' = H, 1-10C alkyl (optionally substituted by halogen, OH, amino, SH or COOH), aryl (optionally substituted by halogen, OH, amino, SH or COOH), OH, halogen, amino, amide or COOH; m = 0-4; x = the number of positive charges on M; y = the number of negative charges on the cyclic peptide; z = 1 or 2; Kat = a cation; R1, R2, R4, R5 = R; R3 = alkyl or aryl. Independent claims are also included for the following: (1) production of a complex of formula (II) by reacting (IIIa) or (IIIb) with a transition metal salt or complex in the presence of a base and precipitating the complex with a compound containing a suitable cation; (2) a complex of formula (IIa) where M is palladium or nickel: (IIa)
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机译：环状四肽（I）的制备包括在碱的存在下，通过使二肽酯（IIIa）或四肽酯（IIIb）与过渡金属盐或络合物反应，形成环四肽络合物（II），使该络合物与环己酸酯沉淀。含有合适阳离子的化合物，通过与质子酸反应从配合物中释放（I），并分离（I）。反应中使用的化合物具有下式：Kat（x + zy）+ <= Mx +（C（R）（CHR'）mC（O）N-（C（R）（CHR'）mC（O）N-） 2C（R）（CHR'）mC（O）N）yz→（x-zy）-（II）M =过渡金属离子; R ＝ H或任选地被OH，氨基，COOH和/或酰胺基取代的有机基团; R′＝ H，1-10C烷基（任选地被卤素，OH，氨基，SH或COOH取代），芳基（任选地被卤素，OH，氨基，SH或COOH取代），OH，卤素，氨基，酰胺或COOH; m = 0-4; x = M上的正电荷数; y =环状肽上的负电荷数; z = 1或2; Kat =阳离子; R1，R2，R4，R5 = R; R 3 ＝烷基或芳基。还包括以下方面的独立权利要求：（1）通过使（IIIa）或（IIIb）与过渡金属盐或配合物在碱的存在下反应并用化合物沉淀该配合物来制备式（II）的配合物含有合适的阳离子; （2）其中M是钯或镍的式（IIa）的配合物：（IIa）
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