CAS: 1738-72-3; (S)-Benzyl 2-Amino-3-Hydroxypropanoate

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CAS号59524-02-6 N-叔丁氧羰基-L-丝氨酸 | CAS号214707-40-1 Tos-Ser-OBn | CAS号56-45-1 L-丝氨酸 | CAS号100-51-6 苯甲醇 | CAS号1738-71-2 benzyl α-amino-... | CAS号6192-52-5 对甲苯磺酸一水合物 | CAS号98-11-3 苯磺酸 | CAS号59524-02-6 N-叔丁氧羰基-L-丝氨酸 | CAS号56-45-1 L-丝氨酸 | CAS号58577-88-1 (S)-(-)-2-氨基-3-... | CAS号67413-26-7 (S)-2-氮丙啶甲酸 苄基 酯

N-叔丁氧羰基-L-丝氨酸置于盐酸体系中,用 二氯甲烷,水 用作溶剂,化学反应 18.0H,反应生成丝氨酸苄酯盐酸盐
参考文献:糖基化 α-叠氮基氨基酸:合成新糖缀合物的多功能中间体
标题:糖基化 α-叠氮基氨基酸:合成新糖缀合物的多功能中间体
摘要:合成了一系列糖基化的 α-叠氮基氨基酸作为新糖缀合物的前体,这是一类用于药物发现和传感器开发的重要生物分子.本文所述的具有合成挑战性的 1,2-顺式 α-半乳糖基化物种被设计为合成 α-半乳糖基神经酰胺类似物的构件,该类似物是一种有效的免疫调节剂.使用叠氮化铜炔环加成反应制备了苄基保护的 1,2,3-三唑基 α-半乳糖基-1-丝氨酸衍生物,以展示糖基化 α-叠氮基氨基酸在新糖缀合物设计中的潜力.
Doi:10.1055/s-0036-1591902

专利信息

专利号:US-5712367-A
优先权日:1989-10-02
标 题:Process for the solubilization of peptides and process for peptide synthesis
发明人：BERNARD JEAN-MARIE; BOUZID KAMEL; GERVAIS CHRISTIAN
权利人:RHONE POULENC CHIMIE
摘要:A process is disclosed for making peptides soluble in a water-immiscible organic solvent, comprising linking a lipophilic group with an amide or ester bond to the terminal carboxyl group of said peptide; when the lipophilic group is linked to L-serine, a molecule is obtained with a solubility in water at 25 DEG C. of less than 30 g/liter. This lipophilic group is non-polymeric and chemically defined. A process is also disclosed for the synthesis of peptides, optionally protected, in a liquid medium, wherein the starting material is an amino acid or peptide made soluble in an organic medium by a lipophilic group A-L linked to the carboxyl function of the starting amino acid or peptide, and are added to amino acids or peptides to be condensed which are activated on their acid function and protected on their amine function and are optionally protected on their side chain. The peptides resulting from the synthesis are used, where appropriate, for the synthesis of medicinal products, vaccines or agri-foodstuff or plant-protection.

专利号:US-4876323-A
优先权日:1984-02-27
标题:α-substituted acrylic acid esters, their polymers and method of synthesizing same
发明人：ENGEL JAMES F; BYERLEY THOMAS J; CHRISTIE HOWARD W
权利人:MIDWEST RESEARCH INST
摘要:α-Substituted acrylic acid esters, their polymers and adhesives therefrom, and methods of synthesizing these compounds. The compounds of the invention are useful as intermediates in the synthesis of isocyanato esters and can be polymerized to form an effective, non-toxic adhesive. The method of the invention encompasses utilizing the adhesive composition in biomedical applications, such as joining live animal tissue. Other adhesive applications are contemplated for living tissue and inanimate objects. The compounds are also used as monomers which can be polymerized, used in conjunction with other monomers as adhesive compositions, cross-linking agents, dye acceptor additives to vinylic polymers and useful chemical intermediates. The method of the invention encompasses synthesizing the aforementioned monomers and intermediates. Methyl α-(ethoxycarbonamido)acrylate is synthesized from either DL-serine or methyl pyruvate. For use as an intermediate, silyl substitution of the compound is accomplished by reacting the ester with trimethylchlorosilane. This α-substituted silated ester is used as an intermediate in the preparation of methyl α-isocyanatoacrylate, which can be polymerized with N-vinyl-2-pyrrolidone to produce a desirable adhesive. Analagous procedures, starting with L-ethyl serine and L-benzyl serine, respectively, are followed to arrive at the corresponding ethyl and benzyl esters.

专利号:US-5175266-A
优先权日:1991-04-19
标 题 :Nucleosides and oligonucleosides with a phosphate-free internucleoside backbone and process for preparing the same
发明人：VARMA RAJENDER S; HOGAN MICHAEL E; REVANKAR GANAPATHI R; RAO TAKKELLAPATI S
权利人:TRIPLEX PHARMA CORP; BAYLOR COLLEGE MEDICINE
摘要:Nucleoside derivatives which contain a nucleo-base, a sugar and an amino acid backbone of the structure: ##STR1## where R' refers to the various amino acid side chains or their blocked equivalent and R refers to a nucleo-base or its blocked equivalent. The synthesis of these nucleoside derivatives proceeds by a series of steps including oxidation of the 3'-azido nucleoside derivative, coupling to a benzylated ester of an amino acid to yield the amide and hydrogenation. The adenine, guanine, cytosine and thymine nucleosides with an amino acid at the 5' terminus are synthesized. From such monomers oligonucleotides can be synthesized which possess an amino acid backbone, using either solid state phase chemistry or liquid phase chemistry.

专利号:US-4704466-A
优先权日:1984-02-27
标题:α-substituted acrylic acid esters
发明人：ENGEL JAMES F; BYERLEY THOMAS J; CHRISTIE HOWARD W
权利人:MIDWEST RESEARCH INST
摘要:α-Substituted acrylic acid esters, their polymers and adhesives therefrom, and methods of synthesizing these compounds. The compounds of the invention are useful as intermediates in the synthesis of isocyanato esters and can be polymerized to form an effective, non-toxic adhesive. The method of the invention encompasses utilizing the adhesive composition in biomedical applications, such as joining live animal tissue. Other adhesive applications are contemplated for living tissue and inanimate objects. The compounds are also used as monomers which can be polymerized, used in conjunction with other monomers as adhesive compositions, cross-linking agents, dye acceptor additives to vinylic polymers and useful chemical intermediates. The method of the invention encompasses synthesizing the aformentioned monomers and intermediates. Methyl α-(ethoxycarbonamido)acrylate is synthesized from either DL-serine or methyl pyruvate. For use as an intermediate, silyl substitution of the compound is accomplished by reacting the ester with trimethylchlorosilane. This α-substituted silated ester is used as an intermediate in the preparation of methyl α-isocyanatoacrylate, which can be polymerized with N-vinyl-2-pyrrolidone to produce a desirable adhesive. Analagous procedures, starting with L-ethyl serine and L-benzyl serine, respectively, are followed to arrive at the corresponding ethyl and benzyl esters.

专利号:US-8153100-B2
优先权日:2007-01-11
标题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
发明人：MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of 18 F or 19 F labeled molecules of use in PET or MRI imaging. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled. Preferably, the 18 F or 19 F is conjugated to a targeting molecule by formation of a metal complex and binding of the 18 F- or 19 F-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the 18 F or 19 F bound to the metal. In other embodiments, the 18 F or 19 F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The 18 F or 19 F labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET or MRI imaging.

专利号:US-8147800-B2
优先权日:2007-01-11
标 题 :Methods and compositions for F-18 labeling of proteins, peptides and other molecules
发明人：MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M
权利人:MCBRIDE WILLIAM J; D SOUZA CHRISTOPHER A; GOLDENBERG DAVID M; IMMUNOMEDICS INC
摘要:The present application discloses compositions and methods of synthesis and use of F-18 labeled molecules of use, for example, in PET imaging techniques. The labeled molecules may be peptides or proteins, although other types of molecules may be labeled by the described methods. Preferably, the F-18 may be conjugated to a targeting molecule by formation of a metal complex and binding of the F-18-metal complex to a chelating moiety. Alternatively, the metal may first be conjugated to the chelating group and subsequently the F-18 bound to the metal. In other embodiments, the F-18 labeled moiety may comprise a targetable construct used in combination with a bispecific or multispecific antibody to target F-18 to a disease-associated antigen, such as a tumor-associated antigen. The F-18 labeled targetable construct peptides are stable in serum at 37° C. for a sufficient time to perform PET imaging analysis.