CAS: 3057-74-7; H-Asp(Otbu)-Oh

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64960-75-4 112883-39-3 1676-90-0

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(2R)-N-[(2S)-2-[[bis(Methylthio)Methylidene]Amino]-3-[(Tert-Butyl)Oxycarbonyl]Propan-1-Oyl]Bornane-10,2-Sultam置于三氟乙酸体系中,化学反应 2.0H,以75%的收率获得产物l-天门冬氨酸-4-叔丁基酯
参考文献:苏丹娜衍生的甘氨酸等效物的不对称烷基化:对映体纯α-氨基酸的实际制备
标题:苏丹娜衍生的甘氨酸等效物的不对称烷基化:对映体纯α-氨基酸的实际制备
摘要:磺胺衍生的n-[双(甲基)硫代亚甲基]甘氨酸酯等效物的去质子化/烷基化得到结晶产物,其在温和水解下以高总收率提供α-氨基酸(〜100%ee).
DOI:10.1016/s0040-4039(01)93840-7

专利信息

专利号:US-5124478-A
优先权日:1987-12-22
标 题:Acid-labile anchor groups for the synthesis of peptide amides by a solid-phase method
发明人：BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER
权利人:HOECHST AG
摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl, R 2 denotes an amino acid residue which is protected with a urethane protective group which can be eliminated with weak acid or base, or denotes an amino protective group which can be eliminated with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or --O--(CH 2 ) n --COOH (with n=1 to 6), with one of these radicals being --O--(CH 2 ) n --COOH, or Y 1 , Y 2 and Y 5 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl or (C 1 -C 4 )-alkoxy, Y 3 denotes hydrogen or (C 1 -C 8 )-alkoxy and Y 4 denotes --(CH 2 ) n --COOH or --NH--CO--(CH 2 ) n --COOH (with n=1 to 6). n Processes for the preparation thereof and the synthesis of peptide amides by a solid-phase method using these new compounds (spacers) are described.

专利号:US-7960578-B2
优先权日:2007-03-21
标题:Method for the synthesis of peptides without solvent
发明人：MARTINEZ JEAN; LAMATY FREDERIC; DECLERCK VALERIE
权利人:CENTRE NAT RECH SCIENT; UNIV MONTPELLIER I
摘要:The disclosure relates to a method for the synthesis of a compound of the formula (I) in which: n is an integer higher than or equal to 1; Rb and each Rn are independently a hydrogen atom, a C 1 -C 6 arylalkyl group or a C 1 -C 6 alkyl group substituted or not by an aryl group, —COOH, C 1 -C 6 , —COO-(alkyl), —CONH 2 , —SH, heteroaryl, —NH 2 , —NHC(NH)(NH 2 ), C 1 -C 6 -s-(alkyl), —OH or phenol; Ra is a N-protective group; Rc is a ORd group in which Rd is a C 1 -C 6 alkyl group or a NReRf group in which Re and Rf Re independently an N-protective group.

专利号:US-4922015-A
优先权日:1987-04-08
标 题:Synthesis of peptide amides by means of a solid phase method using acid-labile anchoring groups
发明人：BREIPOHL GERHARD; KNOLLE JOCHEN; STUEBER WERNER
权利人:HOECHST AG
摘要:The invention relates to new compounds of the formula ##STR1## in which R 1 denotes (C 1 -C 8 )-alkyl or optionally substituted (C 6 -C 14 )-aryl, R 2 denotes hydrogen or an amino acid residue which is protected by an amino protective group which can be cleaved off with weak acid or base, R 3 denotes hydrogen or (C 1 -C 4 )-alkyl, and Y 1 -Y 9 denote identical or different radicals hydrogen, (C 1 -C 4 )-alkyl, (C 1 -C 4 )-alkoxy or -O-(CH 2 ) n -COOH (with n=1 to 6), one of these radicals being -O-(CH 2 ) n -COOH. A process for the preparation thereof and the synthesis of peptide amides by means of a solid phase method using these new compounds (spacers) are described.

专利号:US-5565606-A
优先权日:1986-10-21
标 题:Synthesis of peptide aminoalkylamides and peptide hydrazides by the solid-phase method
发明人：BREIPHOL GERHARD; KNOLLE JOCHEN
权利人:HOECHST AG
摘要:The invention relates to compounds of the formula I in which A denotes hydrogen or an amino protective group, B denotes one or more amino acids, X denotes alkylene or aralkylene, Y1, Y2, Y3 and Y4 are identical or different and denote hydrogen, methyl, methoxy or nitro, V denotes hydrogen or a carboxyl protective group, W denotes -[CH2]n- or -O-[CH2]n-, m denotes 0 or 1, n denotes 0 to 6, and p denotes 0 to 5, to a process for their preparation. The compounds of formula I are useful as linkage agents or anchor groups in the solid-phase synthesis of peptide aminoalkylamides and peptide hydrazides.

专利号:US-6849710-B1
优先权日:1996-07-30
标 题:Method for the synthesis of analogs of parathyroid hormone and parathyroid hormone related peptide
发明人：ARZENO HUMBERTO
权利人:HOFFMANN LA ROCHE
摘要:A fragment condensation process for the synthesis of analogs of parathyroid hormone (PTH) and parathyroid hormone related peptide (PTHrP), in which amino acid residues (22-31) form a synthetic amphipathic α-helix, is provided.

专利号:US-4504415-A
优先权日:1983-04-04
标题:Synthesis of thymosin α1 and desacetyl thymosin α1
发明人：FELIX ARTHUR M; GILLESSEN DIETER; STUDER ROLF; MEIENHOFER JOHANNES A; TRZECIAK ARNOLD
权利人:HOFFMANN LA ROCHE
摘要:An improved solution phase synthesis of thymosin alpha 1 and desacetyl thymosin alpha 1 with t-Boc side chain protection and proceeding through novel intermediates is disclosed.