38308-92-8Relevant articles and documents
Synthesis method of 2,4-diaminobutyric acid derivative
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Paragraph 0071-0073, (2021/03/11)
The invention belongs to the field of organic chemistry, and particularly relates to a synthesis method of a 2,4-diaminobutyric acid derivative. According to the synthesis method of the 2,4-diaminobutyric acid and the derivative thereof provided by the invention, homoserine is selected as an initial raw material, the amino and carboxyl of the homoserine are protected firstly, a pht group is introduced through a light delay reaction, and then a final product can be obtained through six steps of benzyl ester removal, pht removal and Boc group removal. According to the invention, the synthetic method provided by the invention has relatively high reaction yield and is convenient for separation and purification; the intermediates obtained in the reaction are all protecting group modified aminoacid derivatives and can be directly used as drug intermediates or raw materials for synthesizing other compounds, so that waste is avoided; and the reaction conditions provided by the invention are mild, and later-period amplification production is facilitated.
HETEROCYCLIC COMPOUNDS AS PRMT5 INHIBITORS
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Paragraph 000148, (2019/06/11)
The compounds of Formula I, Formula Ia, and Formula Ib are described herein along with their analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites, and prodrugs thereof. These compounds inhibit PRMT5 and are useful as therpeautic or ameliorating agent for diseases that are involved in cellular growth such as malignant tumors, schizophrenia, Alzheimer's disease, Parkinson's disease and the like.
TETRAHYDROPYRIDOPYRIMIDINES AND TETRAHYDROPYRIDOPYRIDINES AS INHIBITORS OF HBSAG (HBV SURFACE ANTIGEN) AND HBV DNA PRODUCTION FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTIONS
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Page/Page column 149; 150, (2016/11/21)
The present invention provides tetrahydropyridopyrimidines and tetrahydropyridopyridines having the general formula (I) wherein R1, R2, U, W, X, Y and Z are as described herein, as inhibitors of HBsAg (HBV surface antigen) and HBV DNA production for the treatment and prophylaxis of hepatitis B virus infections.
AMIDE COMPOUND AND MEDICINAL USE THEREOF
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Page/Page column 101, (2013/02/27)
A compound of formula [I-W]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
Structure-activity study of new inhibitors of human betaine-homocysteine S-methyltransferase
Vaněk, Václav,Budě?ínsky, Milo?,Kabeleová, Petra,?anda, Miloslav,Koz?í?ek, Milan,Han?lová, Ivona,Mládková, Jana,Brynda, Ji?í,Rosenberg, Ivan,Koutmos, Markos,Garrow, Timothy A.,Jirá?ek, Ji?í
supporting information; experimental part, p. 3652 - 3665 (2010/04/30)
Betaine-homocysteine S-methyltransferase (BHMT) catalyzes the transfer of a methyl group from betaine to L-homocysteine, yielding dimethylglycine and L-methionine. In this study, we prepared a new series of BHMT inhibitors. The inhibitors were designed to mimic the hypothetical transition state of BHMT substrates and consisted of analogues with NH, N(CH3), or N(CH 3)2 groups separated from the homocysteine sulfur atom by a methylene, ethylene, or a propylene spacer. Only the inhibitor with the N(CH3) moiety and ethylene spacer gave moderate inhibition. This result led us to prepare two inhibitors lacking a nitrogen atom in the S-linked alkyl chain: (RS,RS)-5-(3-amino-3-carboxypropylthio)-3-methylpentanoic acid and (RS)-5-(3-amino-3-carboxypropylthio)-3,3-dimethylpentanoic acid. Both of these compounds were highly potent inhibitors of BHMT. The finding that BHMT does not tolerate a true betaine mimic within these inhibitors, especially the nitrogen atom, is surprising and evokes questions about putative conformational changes of BHMT upon the binding of the substrates/products and inhibitors.
Novel acyl-dipeptide-like compounds, a method for preparing the same and pharmaceutical compositions containing such products
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Page/Page column 5, (2008/06/13)
The invention relates to the field of chemistry and more specifically to the field of medicinal chemistry. The invention is directed to N-acyl-dipeptide-like compounds having the general formula I wherein substituents A, B, X, Y, R1, R2, and subscripts n, m, p and q have the same meanings as those given in the claims. The invention is equally directed to pharmaceutical compositions containing as an active ingredient at least one compound of general formula I either in acid or salt form with an organic or mineral base. The compounds persuant to the invention display interesting pharmacological properties which make them useful as drugs.
Cyclic hydroxamates, especially multiply substituted [1,2]oxazinan-3-ones
Wolfe, Saul,Wilson, Marie-Claire,Cheng, Ming-Huei,Shustov, Gennady V.,Akuche, Christiana I.
, p. 937 - 960 (2007/10/03)
Routes to putative N-acyl-D-ala-D-ala surrogates, beginning with the conversion of 4-, 5-, and 6-membered lactones into 5-, 6-, and 7-membered cyclic hydroxamates, are reported. The key step of the synthesis is trimethylaluminium-promoted cyclization of an ω-aminooxyester. The 7-membered cyclic hydroxamate crystallizes in a chair conformation. Extension of the reaction sequence to homoserine or homoserine lactone leads to cyclocanaline and N-acylated cyclocanalines. The 4-phenylacetamido derivative of cyclocanaline crystallizes in a boat conformation. The attachment of a 2-carboxypropyl substituent to the ring nitrogen of a 4-acylaminocyclocanaline has been effected, prior to cyclization, by coupling of the acyclic aminooxyester precursor to the triflate of benzyl lactate or, after cyclization, by coupling to tert-butyl α-bromopropionate in the presence of potassium fluoride - alumina, followed by removal of the protecting group in each case. A six-membered homolog of the antibiotic lactivicin has been synthesized by the reaction of 4-phenylacetamidocyclocanaline with benzyl 2-oxoglutarate in the presence of carbodiimide, followed by hydrogenolysis. Starting with methyl 2,4-dibromo-2,4-dideoxy-L-erythronate, which is available in two steps from L-ascorbic acid, these reaction sequences have been applied to the stereospecific synthesis of a D-alanine derivative whose nitrogen atom is enclosed within a 3,4-disubstituted [1,2]oxazinan-3-one.
Cephalosporin derivatives
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, (2008/06/13)
This is a class of antibacterial compounds of the formula: STR1 wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group STR2 wherein n is 0 or an integer of 1-3, A is a group --COR3 wherein R3 is hydroxy, a group STR3 wherein R4 and R5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group STR4 or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R1 and R2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R1 and R2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: STR5 wherein m is 0 or an integer of 3-5, R6 is hydrogen or alkyl of 1-3 carbon atoms, and R7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH2)p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group STR6 wherein R8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.