143868-89-7Relevant academic research and scientific papers
Preparation method of (R)-4-propyl-dihydrofuran-2-one and preparation intermediate of (R)-4-propyl-dihydrofuran-2-one
-
Paragraph 0047-0048, (2020/07/14)
The invention discloses a preparation method of (R)-4-propyl-dihydrofuran-2-one and a preparation intermediate of (R)-4-propyl-dihydrofuran-2-one. The preparation method of the intermediate comprisesthe following steps: (1) in the presence of an acid or an alkali, carrying out hydrolysis reaction on a compound I to obtain a compound II or a salt thereof; and (2) carrying out reduction reaction onthe compound II or the salt thereof and a reducing agent to obtain a compound III. According to the preparation route disclosed by the invention, the use of flammable and explosive reaction reagentsin the existing route is avoided; reagents which are low in cost and easy to obtain in industry are used; compared with the prior art, the method has the advantages of low cost, safety in production,realization of the purification and the separation of the intermediate by using the acid-base property of the compound and adopting the mode of adjusting the pH value of the system in the reaction process and the post-treatment operation, avoiding of recrystallization, filtration and other tedious operation modes, simplification of the operation, and suitableness for industrial large-scale production.
A (R)-4 - propyl - dihydrofuran -2 - ketone
-
Paragraph 0076-0085, (2019/04/10)
The invention discloses a process for preparing (R)- 4 - propyl - dihydrofuran - 2 - one method, the key intermediate type B compound, type C compound and its preparation method; (R)- 4 - propyl - dihydrofuran - 2 - one of the preparation method of the operability of the strong, is suitable for industrial production.
PROCESS FOR PREPARING OPTICALLY PURE (R)-4-N-PROPYL-DIHYDROFURAN-2(3H)-ONE
-
Paragraph 0080-0082, (2019/12/10)
The present invention discloses a process for preparing optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one, belonging to the field of chemical synthesis. According to the process, optically pure (S)-3-n-pentanoyl-4-substituted oxazol-2-one is used as a starting material, and after alkylation, reduction, cyano hydrolysis, lactonization, the product optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one is given. The preparation process has the advantages of easy availability of raw materials, low price, high yield, high optical purity of product, simple reaction conditions and simple operations.
Optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method
-
Paragraph 0104-0106, (2018/09/28)
The present invention relates to an optically pure (R)-4-n-propyl-dihydrofuran-2(3H)-one preparation method, wherein optically pure (S)-3-n-pentanoyl-4-substituted oxazole-2-one is used as a raw material, alkylation reaction with an olefin or alkyne reagent, reducing removal of a chiral auxiliary group, oxidation of double bond or triple bond and other steps are performed to prepare the opticallypure (R)-4-n-propyl-dihydrofuran-2(3H)-one. According to the present invention, the preparation method has characteristics of easily available raw material, low cost, high total yield, high optical purity of the obtained product, simple reaction conditions and simple operation process.
New synthesis method of brivaracetam
-
Paragraph 0057; 0058; 0059; 0060, (2017/10/13)
The invention provides a synthesis method of brivaracetam. The method adopts cheap and easily available pentanoic acid or valeryl halide as an initial raw material, and provides a brand new synthesis route of a brivaracetam medicine, and the whole reaction route has a high total yield. The method has the advantages of high productivity, low cost, and suitableness for large-scale industrial production.
Method for preparing chiral 4-substituted dihydrofuran-2(3H)-ketone
-
Paragraph 0044; 0045; 0046; 0047, (2017/06/02)
The invention provides a method for preparing chiral 4-substituted dihydrofuran-2(3H)-ketone. The method comprises the following steps: (a) dropwise adding acyl chloride (3) into an organic solvent solution of a compound (1), enabling reaction to obtain an acyl chloride intermediate solution, then dropwise adding an organic solvent solution of a compound (2) and enabling reaction to obtain a compound (4); (b) dropwise adding a bis(trimethylsilyl)amide alkali metal salt solution into an organic solvent solution of the compound (4), enabling reaction, dropwise adding a compound (5) into the obtained reaction liquid and enabling reaction to obtain a compound (6); (c) enabling reaction between the compound (6) and alkali to obtain a compound (7); (d) enabling reaction between the compound (7) and a reducing agent to obtain a compound (8), wherein R is selected from aryl, arylmethyl or alkyl, R1, R2 and R3 are independently selected from alkyl, and X is selected from Cl, Br or I. The method is simple in process, strong in operability and easy for industrial production. The reaction route is shown in the description.
NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF
-
Page/Page column 187-188, (2014/09/29)
The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.
MACROCYCLIC INHIBITORS OF FLAVIVIRIDAE VIRUSES
-
Page/Page column 70; 71, (2014/01/08)
Provided are compounds of Formula I and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.
Design, synthesis, and biological activity of isophthalic acid derivatives targeted to the C1 domain of protein kinase C
Af Genn?s, Gustav Boije,Talman, Virpi,Aitio, Olli,Ekokoski, Elina,Finel, Moshe,Tuominen, Raimo K.,Yli-Kauhaluoma, Jari
supporting information; experimental part, p. 3969 - 3981 (2010/01/16)
Protein kinase C (PKC) is a widely studied molecular target for the treatment of cancer and other diseases. We have approached the issue of modifying PKC function by targeting the C1 domain in the regulatory region of the enzyme. Using the X-ray crystal structure of the PKC δ C1b domain, we have discovered conveniently synthesizable derivatives of dialkyl 5-(hydroxymethyl)isophthalate that can act as potential C1 domain ligands. Structure-activity studies confirmed that the important functional groups predicted by modeling were indispensable for binding to the C1 domain and that the modifications of these groups diminished binding. The most promising compounds were able to displace radiolabeled phorbol ester ([3H]PDBu) from PKC α and δ at Ki values in the range of 200-900 nM. Furthermore, the active isophthalate derivatives could modify PKC activation in living cells either by inducing PKC-dependent ERK phosphorylation or by inhibiting phorbol-induced ERK phosphorylation. In conclusion, we report here, for the first time, that derivatives of isophthalic acid represent an attractive novel group of C1 domain ligands that can be used as research tools or further modified for potential drug development.
An efficient synthetic approach towards trans-β2,3-amino acids and demonstration of their utility in the design of therapeutically important β2,3-peptides and α,β2,3-peptide aldehydes
Balamurugan, Dhayalan,Muraleedharan, Kannoth M.
supporting information; experimental part, p. 10074 - 10082 (2010/02/27)
An efficient synthetic approach towards trans-β2,3-amino acids involving anti-selective aldol, azidation and controlled hydrolysis as key steps is discussed. Apart from structural elaboration of these building blocks to homo- and hetero-dipepti
