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44 results about "Norvaline" patented technology

Norvaline (abbreviated as Nva) is an amino acid with the formula CH₃(CH₂)₂CH(NH₂)CO₂H. The compound is an isomer of the more common amino acid valine. Like most other α-amino acids, norvaline is chiral. It is a white, water-soluble solid.

Method for determining other amino acids in L-valine raw material by high performance liquid chromatography

ActiveCN111505151ASolve the problem of short service life and unstable baseline of reversed phaseEasy to separateComponent separationSilica gelPhenylalanine
The invention provides a method for determining other amino acids in an L-valine raw material by high performance liquid chromatography. The method comprises the following steps of preparing L-valine,leucine, isoleucine, glycine, alanine and phenylalanine reference substance solutions; detecting through a high performance liquid chromatograph, comparing the appearance time and peak shape of L-valine, leucine, isoleucine, glycine, alanine and phenylalanine in a chromatogram of the test sample with those of L-valine, leucine, isoleucine, glycine, alanine and phenylalanine in a chromatogram of the reference substance solution, and judging whether the test sample solution contains other amino acids or not. According to the method, by screening an aminopropyl bonded silica gel chromatographiccolumn, the separation effects are found, and by screening the wavelengths, the maximum absorption of each amino acid is found, and the retention time of each amino acid peak on the chromatographic column is regulated and controlled by regulating the ratio of triethylamine, the pH value and the ratio of two phases by utilizing an acetonitrile/phosphate buffer solution binary mobile phase, so thatthe hydrolysis and shedding of bonded aminopropyl in the amino column are effectively prevented, and the problems of short reverse-phase service life and unstable baseline of the amino column are solved.
Owner:宜昌三峡普诺丁生物制药有限公司

Synthesis of D,L-norvaline

The invention discloses a method for synthesizing D, L-norvaline with n-pentanoic acid as a main initial raw material, orderly comprising the following steps: 1) bromo reaction: n-pentanoic acid is reacted with liquid bromine to form alpha-bromo n-pentanoic acid; 2) ammonolysis: the obtained alpha-bromo n-pentanoic acid is firstly neutralized by strong aqua ammonia under the protection of nitrogen and under ice bath cooling, and then is ammonolyzed for 0.5 to 12 hours at a temperature between 40 and 90 DEG C by using ammonia water or ammonia gas as an ammonolysis reagent and hexamethylenetetramine as a catalyst; then the obtained suspension is filtered, and the filtering cake is washed by methanol or ethanol and dried to form the D, L-norvaline; and 3) ion exchange to separate and recycle: the obtained filtrate in the step of ammonolysis and cation exchange resin are subjected to ion exchange, and materials on the resin are eluted with weak aqua ammonia, decolored, dewatered, washed by methanol or ethanol and dried to form the D, L-norvaline. The D, L-norvaline obtained in step 2) and step 3) is combined, and the ammonolysis yield is over 95 percent. The method for synthesizing the D, L-norvaline has advantages of simple process, few reaction steps, high yield, low cost, short production period and the like. The obtained D, L-norvaline can be further subjected to chemical resolution or enzymatic resolution to form chiral norvaline.
Owner:吕亮

Radiolabeled melanocortin 1 receptor-specific alpha-melanocyte-stimulating hormone analogues for imaging or therapy

A compound is provided comprising a melanocortin 1 receptor (MC1R) targeting peptide (MC1RTP), a radiolabeling group, and a linker joining the MC1RTP to the radio labeling group. The MC1RTP is linear or cyclized, and comprises a sequence of Formula I or Formula II: Xaa1-Xaa2a-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7a (I) or Xaa1-Xaa2b-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7b (II). Xaa1 is L- / D-Nle, L- / D-Nle, L- / D-Ala, L- / D-Leu, L- / D-Ile, D-Ile, L- / D-Cys, L- / D-Met, L- / D-Phe, L- / D-Trp, L- / D-Val, L- / D-Nal, L- / D-2-Nal, Gly, L- / D-α-aminobutryic acid, L- / D-norvaline, or L- / D-homonorleucine. Xaa2a and Xaa7b are L- / D-Cys, L- / D-Asp, L- / D-Glu, L- / D-2-Aad, L- / D-3-Aad, L- / D-Pra, L- / D-Hpg, or L- / D-Bpg. Xaa2b and Xaa7a are L- / D-Cys, L- / D-Lys, L- / D-Orn, L- / D-Dab, L- / D-Dap, L- / D-Lys(N3), L- / D-Orn(N3), L- / D-Dab(N3), L- / D-Dap(N3), L- / D-2-(5′-azidopentyl)alanine, or L- / D-2-(6′-azidohexyl)alanine. Xaa3 is L- / D-His, Pro, beta-(1,2,3-triazol-4-yl)-L-alanine, beta-(1,2,3-triazol-4-yl)-D-alanine, 1,2,4-triazole-3-alanine, or 1,2,4-triazole-3-D-alanine. Xaa4 is L- / D-Phe, L- / D-2-Nal, L- / D-Phe(4-F), L- / D-Phe(4-Cl), L- / D-Phe(4-Br), L- / D-Phe(4-I), L- / D-Phe(4-NH2), or L- / D-Phe(4-NO2). Xaa5 is L- / D-Arg, L- / D-hArg), Leu, L- / D-Agb, or L- / D-Agp. Xaa6 is L- / D-Trp, L- / D-Phe, L- / D-Trp(5-Br), L- / D-Trp(5-OCH3), L- / D-Trp(6-F), L- / D-Trp(5-OH) or L- / D-Trp(CHO). One or more amino acid residues of the MC1RTP is alpha N-methylated, wherein 1, 2, 3 or 4 of Xaa3, Xaa5, Xaa6 and Xaa7a is alpha N-methylated or wherein 1, 2, 3 or 4 of Xaa3, Xaa5, Xaa6 and Xaa7b is alpha N-methylated. The linker comprises an albumin-binding group.
Owner:PROVINCIAL HEALTH SERVICES AUTHORITY

Method for synthesizing L-norvaline

The invention provides a method for synthesizing L-norvaline. The method comprises the following steps: 1, adding acetic acid into a reaction kettle, adding DL-norvaline and D-tartaric acid while stirring, heating to 80DEG C, adding salicylaldehyde, and maintaining the temperature in a range of 80-85DEG C for 10h; 2, cooling to 20-25DEG C after temperature maintenance, keeping the decreased temperature for 1h, and centrifuging to obtain crude L-norvaline and D-tartaric acid; 3, adding petroleum ether to the crude L-norvaline and D-tartaric acid, stirring and washing for 30min, and centrifuging to obtain a purified L-norvaline and D-tartaric acid double salt; 4, heating the double salt in water to 70DEG C in order to completely dissolve the double salt, adjusting the pH value to 7 by using ammonia water, cooling to 20-25DEG C, crystallizing for 2h, centrifuging, and rinsing by using methanol to obtain crude L-norvaline; and 5, heating the crude L-norvaline in water to 80-85DEG C in order to completely dissolve the crude L-norvaline, adding active carbon, decoloring for 1h, filtering, concentrating, cooling to 20-25DEG C, crystallizing for 3h, centrifuging, rinsing with water to obtain wet L-norvaline, and carrying out 60DEG C vacuum drying to obtain dry L-norvaline. The method has the advantages of few steps, good environmental protection property and high yield.
Owner:NANJING REDWOOD FINE CHEM CO LTD

Radiolabeled melanocortin 1 receptor-specific alpha-melanocyte-stimulating hormone analogues for imaging or therapy

A compound is provided comprising a melanocortin 1 receptor (MC1R) targeting peptide (MC1RTP), a radiolabeling group, and a linker joining the MC1RTP to the radiolabeling group. The MC1RTP is linear or cyclized, and comprises a sequence of Formula I or Formula II: Xaa1-Xaa2a-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7a (I) or Xaa1-Xaa2b-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7b (II). Xaa1 is L- / D-Nle, L- / D-Nle, L- / D-Ala, L- / D-Leu, L- / D-Ile, D-Ile, L- / D-Cys, L- / D-Met, L- / D-Phe, L- / D-Trp, L- / D-Val, L- / D-Nal, L- / D-2-Nal, Gly, L- / D-α-aminobutryic acid, L- / D-norvaline, or L- / D-homonorleucine. Xaa2a and Xaa7b are L- / D-Cys, L- / D-Asp, L- / D-Glu, L- / D-2-Aad, L- / D-3-Aad, L- / D-Pra, L- / D-Hpg, or L- / D-Bpg. Xaa2b and Xaa7a are L- / D-Cys, L- / D-Lys, L- / D-Orn, L- / D-Dab, L- / D-Dap, L- / D-Lys(N3), L- / D-Orn(N3), L- / D-Dab(N3), L- / D-Dap(N3), L- / D-2-(5′-azidopentyl)alanine, or L- / D-2-(6′-azidohexyl)alanine. Xaa3 is L- / D-His, Pro, beta-(1,2,3-triazol-4-yl)-L-alanine, beta-(1,2,3-triazol-4-yl)-D-alanine, 1,2,4-triazole-3-alanine, or 1,2,4-triazole-3-D-N alanine. Xaa4 is L- / D-Phe, L- / D-2-Nal, L- / D-Phe(4-F), L- / D-Phe(4-Cl), L- / D-Phe(4-Br), L- / D-Phe(4-I), L- / D-Phe(4-NH2), or L- / D-Phe(4-NO2). Xaa5 is L- / D-Arg, L- / D-hArg), Leu, L- / D-Agb, or L- / D-Agp. Xaa6 is L- / D-Trp, L- / D-Phe, L- / D-Trp(5-Br), L- / D-Trp(5-OCH3), L- / D-Trp(6-F), L- / D-Trp(5-OH) or L- / D-Trp(CHO). One or more amino acid residues of the MC1RTP is alpha N-methylated, wherein 1, 2, 3 or 4 of Xaa3, Xaa5, Xaa6 and Xaa7a is alpha N-methylated or wherein 1, 2, 3 or 4 of Xaa3, Xaa5, Xaa6 and Xaa7b is alpha N-methylated. The linker comprises an albumin-binding group.
Owner:PROVINCIAL HEALTH SERVICES AUTHORITY

Synthesis of D,L-norvaline

The invention discloses a method for synthesizing D, L-norvaline with n-pentanoic acid as a main initial raw material, orderly comprising the following steps: 1) bromo reaction: n-pentanoic acid is reacted with liquid bromine to form alpha-bromo n-pentanoic acid; 2) ammonolysis: the obtained alpha-bromo n-pentanoic acid is firstly neutralized by strong aqua ammonia under the protection of nitrogen and under ice bath cooling, and then is ammonolyzed for 0.5 to 12 hours at a temperature between 40 and 90 DEG C by using ammonia water or ammonia gas as an ammonolysis reagent and hexamethylenetetramine as a catalyst; then the obtained suspension is filtered, and the filtering cake is washed by methanol or ethanol and dried to form the D, L-norvaline; and 3) ion exchange to separate and recycle: the obtained filtrate in the step of ammonolysis and cation exchange resin are subjected to ion exchange, and materials on the resin are eluted with weak aqua ammonia, decolored, dewatered, washed by methanol or ethanol and dried to form the D, L-norvaline. The D, L-norvaline obtained in step 2) and step 3) is combined, and the ammonolysis yield is over 95 percent. The method for synthesizing the D, L-norvaline has advantages of simple process, few reaction steps, high yield, low cost, short production period and the like. The obtained D, L-norvaline can be further subjected to chemical resolution or enzymatic resolution to form chiral norvaline.
Owner:吕亮
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