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公开(公告)号:US5028693A
公开(公告)日:1991-07-02
申请号:US379111
申请日:1989-07-13
IPC分类号: C07D263/44 , C07D277/34 , C07K1/02 , C07K1/04
CPC分类号: C07D263/44 , C07D277/34 , C07K1/023 , C07K1/04
摘要: Urethane-protected NCAs and MTAs are prepared by reacting an NCA or NTA with a haloformate in an inert diluent, under anhydrous conditions and in the presence of a tertiary nitrogen-containing base having an atom or functional group sufficiently electron rich and positioned relative to the nitrogen of said base so as to render said atom or group capable of complexing with the H--N
摘要翻译: 氨基甲酸酯保护的NCA和MTA通过使NCA或NTA与卤代甲酸酯在惰性稀释剂中在无水条件下和在具有足够电子富集的原子或官能团的叔氮基的存在下,相对于 所述碱的氮气使所述原子或基团能够与所述N-羧酸酐或N-硫代羧酸酐的HN基团络合,但能够产生能够与卤代甲酸酯反应的N-羧酸酐或N-硫代羧酸酐阴离子络合物。
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公开(公告)号:US4946942A
公开(公告)日:1990-08-07
申请号:US168087
申请日:1988-03-11
IPC分类号: C07D277/20 , C07D263/16 , C07D263/44 , C07D265/06 , C07D267/06 , C07D269/02 , C07D277/34 , C07D279/06 , C07D281/02 , C07D283/02 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07K1/00 , C07K1/02 , C07K1/04 , C07K1/06 , C07K1/113 , C07K5/06 , C07K5/062 , C07K5/08 , C07K5/083
CPC分类号: C07D263/44 , C07D277/34 , C07K1/023 , C07K1/04
摘要: The invention relates to urethane-protected amino acid-N-carboxyanhydride and N-thiocarboxyanhydride compounds which are useful in peptide, polypeptide and protein synthesis. Disclosed herein is the preparation and use of these novel compounds.
摘要翻译: 本发明涉及可用于肽,多肽和蛋白质合成的氨基甲酸酯保护的氨基酸-N-羧酸酐和N-硫代羧酸酐化合物。 本文公开了这些新化合物的制备和用途。
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公开(公告)号:US4362699A
公开(公告)日:1982-12-07
申请号:US242232
申请日:1981-03-10
CPC分类号: B01J19/0046 , B01J2219/00286 , B01J2219/00353 , B01J2219/00418 , B01J2219/00495 , B01J2219/00497 , B01J2219/0059 , B01J2219/00596 , B01J2219/00725 , C40B40/10 , C40B60/14 , Y02P20/582
摘要: An apparatus for synthesizing a polypeptide chain on an insoluble solid support in a continuous flow reactor by performing a series of stepwise coupling reactions under high pressure is disclosed. A deprotecting agent reservoir, a solvent reservoir, a neutralizing solution reservoir, and a plurality of amino acid reservoirs are provided. Each reservoir can be selectively coupled to the reactor and a source of high pressure inert gas or an appropriate pump can be used to force the fluids as needed to the reactor. The reactor also includes a recycle loop whereby the amino acid from a particular reservoir can be recycled through the reactor under high pressure.
摘要翻译: 公开了一种用于在连续流动反应器中通过在高压下进行一系列逐步偶联反应来在不溶性固体载体上合成多肽链的装置。 提供了脱保护剂储存器,溶剂储存器,中和溶液储存器和多个氨基酸储存器。 每个储存器可以选择性地耦合到反应器,并且可以使用高压惰性气体源或适当的泵来迫使反应器所需的流体。 反应器还包括循环回路,其中来自特定储存器的氨基酸可以在高压下再循环通过反应器。
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公开(公告)号:US4351762A
公开(公告)日:1982-09-28
申请号:US242310
申请日:1981-03-10
IPC分类号: C07K1/08 , C07K5/06 , C07K5/103 , C07C103/52
CPC分类号: C07K5/0606 , C07K1/08 , C07K5/101
摘要: In the synthesis of a polypeptide chain wherein an N.sup..alpha. -urethane-protected amino acid mixed anhydride is coupled with an amino-unprotected second amino acid, the improvement comprising conducting said coupling at room temperature or above. This method provides rapid, essentially quantitative reactions without the necessity for reduced temperatures. The method is particularly useful in the solid-phase synthesis of peptides where shortened coupling cycles and improved yields of substantially pure products are obtained.
摘要翻译: 在其中Nα-氨基甲酸酯保护的氨基酸混合酸酐与氨基未受保护的第二氨基酸偶联的多肽链的合成中,改进包括在室温或更高温度下进行所述偶联。 该方法提供快速,基本上定量的反应,而不需要降低温度。 该方法在肽的固相合成中特别有用,其中获得缩短的偶联循环和改进的基本上纯的产物的产率。
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公开(公告)号:US4571345A
公开(公告)日:1986-02-18
申请号:US503853
申请日:1983-06-13
IPC分类号: A23L27/30 , A61K8/44 , A61Q11/00 , C07C13/11 , C07C29/04 , C07C29/40 , C07C45/68 , C07C49/395 , C07C53/128 , C07C53/132 , C07C53/42 , C07C53/44 , C07C61/06 , C07C61/08 , C07C61/15 , C07C233/78 , C07C237/10 , C07C237/50 , C07D331/04 , C07K1/113 , C07K5/06 , C07K5/075 , A23L1/236 , A23L1/226
CPC分类号: C07C29/04 , A61K8/44 , A61Q11/00 , C07C13/11 , C07C29/40 , C07C45/68 , C07C49/395 , C07C53/128 , C07C53/132 , C07C53/42 , C07C53/44 , C07C61/06 , C07C61/08 , C07C61/15 , C07D331/04 , C07C2101/08 , C07C2103/18
摘要: Compounds of the formula: ##STR1## wherein n is 0 or 1, R is lower alkyl (substituted or unsubstituted), R' is H or lower alkyl, and R" is a branched alkyl, alkyl-cycloalkyl, cycloalkyl, polycycloalkyl (poly=2 or more, fused or non-fused), phenyl or alkyl-substituted phenyl, and physiologically acceptable cationic and acid addition salts thereof, which compounds are potent sweeteners. These derivatives of gem-diaminoalkanes are many times sweeter than sugar and are free from undesirable flavor qualities. Furthermore, they possess an unanticipated high degree of solubility compared with known synthetic sweeteners. In addition, the compounds possess high stability so that they can be used in all types of beverages and in conventional food processing. Sweetening compositions and sweetened edible compositions of these compounds are also provided.
摘要翻译: 下式的化合物:其中n为0或1,R为低级烷基(取代或未取代的),R'为H或低级烷基,R“为支链烷基,烷基 - 环烷基,环烷基 ,多环烷基(聚= 2或更多,稠合或未稠合的),苯基或烷基取代的苯基及其生理上可接受的阳离子和酸加成盐,该化合物是有效的甜味剂。 偕二氨基烷烃的这些衍生物比糖更甜,并且没有不良的风味品质。 此外,与已知的合成甜味剂相比,它们具有无法预料的高溶解度。 此外,这些化合物具有高稳定性,因此它们可用于所有类型的饮料和常规的食品加工。 还提供了这些化合物的甜味组合物和甜味食用组合物。
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公开(公告)号:US4829099A
公开(公告)日:1989-05-09
申请号:US74597
申请日:1987-07-17
CPC分类号: C09J175/00 , A61L24/046 , C08G18/16 , C08G18/1833 , C08G18/2018 , C08G18/771 , C08G2170/60 , C08G2230/00
摘要: Metabolically-acceptable, surgical adhesives are prepared from polyisocyanates having the structral formula: ##STR1## wherein R is a polyvalent aliphatic radical of about 1 to 10 carbon atoms or a polyvalent aromatic radical of 6 to about 24 carbon atoms;A is C, S or P;Z is O or S;Y is 1 when A is C or P, and 2 when A is S;n is 1 or 2;p is at least 1;q is 0 or 1, with the proviso that when A is carbon or sulfur, q is 0;r is 0 or 1, with the proviso that when A is carbon or sulfur, r is 0;X is a residue of an organic compound having active hydrogen-containing groups; andX' is a residue of an organic compound having at least 1 active hydrogen-containing group.
摘要翻译: 代谢可接受的手术粘合剂由具有以下结构式的多异氰酸酯制备:其中R是约1-10个碳原子的多价脂肪族基团或6至约24个碳原子的多价芳族基团; A是C,S或P; Z是O或S; 当A为C或P时,Y为1,A为S时为2; n为1或2; p至少为1; q为0或1,条件是当A为碳或硫时,q为0; r为0或1,条件是当A为碳或硫时,r为0; X是具有含活性氢基团的有机化合物的残基; X'是具有至少1个含活性氢基团的有机化合物的残基。
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公开(公告)号:US4192798A
公开(公告)日:1980-03-11
申请号:US962334
申请日:1978-11-20
IPC分类号: B01J19/00 , C07K1/04 , C40B40/10 , C40B60/14 , C07C103/52
CPC分类号: C07K1/045 , B01J19/0046 , B01J2219/00286 , B01J2219/00353 , B01J2219/005 , B01J2219/0059 , B01J2219/00596 , B01J2219/00725 , C40B40/10 , C40B60/14 , Y10S930/29
摘要: In the method for the synthesis of a polypeptide chain on an insoluble solid support wherein an amino acid is introduced into a reactor packed with an insoluble solid support containing substituent groups reactive with said amino acid, coupling said amino acid to said support by condensation reaction with said reactive substituent groups, introducing a second similar or dissimilar amino acid into said reactor and coupling said second amino acid to said first amino acid and repeating the process until the desired polypeptide is obtained, the improvement wherein a high pressure flow system is used and the reaction pressure in said reactor during said synthesis is at least 200 psi up to 10,000 psi or more, in order to obtain rapid reactions and quantitative yields of the desired products.
摘要翻译: 在用于在不溶性固体支持物上合成多肽链的方法中,其中将氨基酸引入填充有与所述氨基酸反应的含有取代基的不溶性固体支持物的反应器中,通过与所述氨基酸的缩合反应将所述氨基酸与所述载体偶联 所述反应性取代基,将第二相似或不相似的氨基酸引入所述反应器并将所述第二氨基酸与所述第一氨基酸偶联并重复所述方法直到获得所需多肽,其改进在于使用高压流动系统, 在所述合成期间所述反应器中的反应压力为至少200psi至10,000psi或更高,以获得所需产物的快速反应和定量产率。
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公开(公告)号:US4125519A
公开(公告)日:1978-11-14
申请号:US731946
申请日:1976-10-13
IPC分类号: C08G69/10
CPC分类号: C08G69/10
摘要: Homopolymers and copolymers containing the amino acid 3,4-dihydroxy-L-phenylalanine (dopa) have been prepared via the synthesis of a protected N-carboxyanhydride (NCA) of the amino acid. These dopa-containing polymers have many uses as in the treatment of Parkinsonism, as drug delivery systems, antioxidants, and fibers and in the production of non-thrombogenic substrates.
摘要翻译: 通过合成氨基酸的保护的N-羧酸酐(NCA)制备含有氨基酸3,4-二羟基-L-苯丙氨酸(多巴)的均聚物和共聚物。 这些含多巴的聚合物在治疗帕金森综合征,药物递送系统,抗氧化剂和纤维以及非血栓形成基质的生产中具有许多用途。
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公开(公告)号:US5631299A
公开(公告)日:1997-05-20
申请号:US461594
申请日:1995-06-05
申请人: Robert J. Kurtz , William D. Fuller
发明人: Robert J. Kurtz , William D. Fuller
CPC分类号: A23L27/40 , A23L27/20 , A23L27/2028 , A23L27/203 , A23L27/204 , A23L27/2052 , A23L27/2054 , A23L27/2056 , A23L27/21 , A23L27/32 , A23L27/33 , A23L27/37 , A23L27/39
摘要: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
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公开(公告)号:US5631292A
公开(公告)日:1997-05-20
申请号:US460581
申请日:1995-06-02
申请人: Robert J. Kurtz , William D. Fuller
发明人: Robert J. Kurtz , William D. Fuller
IPC分类号: A23L27/20 , A23L27/21 , A23L27/30 , A23L27/40 , A61K31/195
CPC分类号: A23L27/40 , A23L27/20 , A23L27/2028 , A23L27/203 , A23L27/204 , A23L27/2052 , A23L27/2054 , A23L27/2056 , A23L27/21 , A23L27/32 , A23L27/33 , A23L27/37 , A23L27/39
摘要: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.
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