40350-82-1Relevant academic research and scientific papers
5-tert-butyloxycarbonyl-2-oxa-5-azabicyclo[2.2.1]heptane-1-carboxylic acid synthesis method
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Paragraph 0008, (2016/10/31)
The present invention relates to a 5-tert-butyloxycarbonyl-2-oxa-5-azabicyclo[2.2.1]heptane-1-carboxylic acid synthesis method. In the prior art, the suitable industrial synthesis method does not exist. A purpose of the present invention is mainly to solve the technical problem in the prior art. The synthesis method comprises six steps, and specifically comprises that a compound 1 and Boc anhydride react under an alkaline condition to obtain a compound 2, the compound 2 is oxidized into a compound 3 by using a 2,2,6,6-tetramethyl piperidine oxide, the compound 3 reacts with a Grignard reagent to obtain a compound 4, the carboxylic acid 4 is reduced with lithium aluminum hydride to obtain a compound 5, the compound 5 reacts with n-butyl lithium and p-tosyl chloride in two stages to obtain a compound 6, and the compound 6 is oxidized with sodium periodate to obtain a final compound 7. The reaction formula is defined in the specification.
POLYMER ORGANOCATALYST AND PREPARATION PROCESS
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, (2011/02/26)
A chiral polymer organocatalyst comprising a main chain and side chain organocatalytic groups covalently attached to the main chain, which organocatalytic groups comprise an amino acid or amino acid derivative of the following general formula (I), in whic
Novel N-substituted alpha aminoacid amides as calcium channel modulators
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, (2008/06/13)
The compounds of formula I and derivatives thereof have been found to be active in tests that show modulation of voltage-dependent calcium channels, and are thus indicated for use in the treatment of diseases in which such modulation is beneficial, in par
Certain phosphonic acids and derivatives
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, (2008/06/13)
The present invention is concerned with the compounds of formula I, wherein one or both of the acidic hydroxy groups of the phos-phonic acid moiety may be etherified, m reprensents one or zero, R1 is carboxy, esterified carboxy or amidated carboxy, wherein the five or six-membered heterocyclic ring may be additionally substituted on carbon and/or nitrogen, may have present a carbon-carbon double bond or may be fused on adjacent carbon atoms with a six-membered carbocyclic ring, A represents a direct bond or lower alkylene provided that A does not represent a direct bond when the heterocyclic ring together with substituent R1 represents 2-carboxypyr-rolidinyl; and salts thereof. These compounds are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excit-atory amino acid receptor.
Certain 2-carboxypiperidyl-alkylene phosphonic acids and esters thereof useful for the treatment of disorders responsive to N-methyl-D-aspartate receptor blockade
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, (2008/06/13)
The present invention is concerned with the phosphonic acids of formula I STR1 wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.
Certain 2-carboxypiperidyl-(alkylene or alkenylene)-phosphonic acids and esters thereof useful for the treatment of disorders responsive to n-methyl-d-aspartate receptor blockade
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, (2008/06/13)
The present invention is concerned with the phosphonic acids of formula I STR1 wherein one or both of the acidic hydroxy groups of the phosphonic acid moiety may be functionalized in form of pharmaceutically acceptable mono- or di- esters; wherein Y represents optionally substituted 2-carboxypyrrolidinyl, 2-carboxy-2,5-dihydropyrrolyl, 2-carboxy-1,2,3,6-tetrahydropyridinyl, 2-carboxy-1,2,5,6-tetrahydropyridinyl, 2-carboxypiperidinyl, 2-carboxytetrahydroquinolinyl or 2-carboxyperhydroquinolinyl, 2-carboxy-2,3-dihydroindolyl or 2-carboxyperhydroindolyl as described herein, and in each of which the carboxy group may be functionalized in form of a pharmaceutically acceptable ester or amide; A represents a direct bond, lower alkenylene, lower alkylidene or lower alkylene provided that A does not represent a direct bond when Y represents 2-carboxypyrrolidinyl; and pharmaceutically acceptable salts thereof; which are useful for the treatment of nervous system disorders in mammals and as antagonists of the N-methyl-D-aspartate sensitive excitatory amino acid receptor.
Method for making substituted prolines
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, (2008/06/13)
A method is provided for making substituted prolines of the structure STR1 wherein X is lower alkyl or aryl, R is H, lower alkyl or an alkali metal and Z is an N-protecting group, which method includes the step of reacting a compound of the structure STR2
