- METHODS OF MAKING WEE1 INHIBITOR COMPOUNDS
-
The invention relates to a method of producing a WEE1 inhibitor of formula (1A) useful in the treatment of pathological conditions characterized by excessive cell proliferation, such as cancer. In some embodiments, the invention relates to methods for producing intermediate compounds of formulas (3), (5) and (6) as defined in the description.
- -
-
Paragraph 0084
(2021/12/31)
-
- Method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane
-
The invention discloses a method for preparing chiral nitrogen-phosphorus ligand L-8 containing pyridocyclopentane, and belongs to the technical field of medical intermediate chiral ligands. The chiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the like in sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiral alcohol preparation is overcome, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adoptedin literature is avoided.
- -
-
-
- Method for synthesizing chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane
-
The invention discloses a method for synthesizing a chiral nitrogen-phosphorus ligand L-8 containing pyridocycloheptane, and belongs to the technical field of medical intermediate chiral ligands. Thechiral nitrogen-phosphorus L-8 ligand is prepared from cyclopentanone through the steps of addition, cyclization, chlorination, asymmetric boronation, oxidation, coupling, esterification and the likein sequence, large-scale preparation is relatively easy to achieve through the route, and the defect that in a traditional route, the yield is low in the first step of ring closing reaction and chiralalcohol preparation, and by selecting a proper chiral ligand, and combining with butyl lithium, asymmetric synthesis of chiral alcohol is realized, and a chiral separation column mode adopted in literature is avoided.
- -
-
-
- GHRELIN O-ACYLTRANSFERASE INHIBITORS
-
This invention relates to novel compounds according to Formula (I) which are inhibitors of ghrelin O-acyltransferase (GOAT), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment
- -
-
Page/Page column 64-66
(2019/08/26)
-
- Production process of 2,3- cyclopenteno pyridine
-
2,3-cyclopenteno pyridine has physiological activity of resisting ulcer and resisting cancer, is an important medical intermediate and alkaloid, is also used for preparing plant protective agents, synthetic resin, antioxidants and the like, and is currently used for the side chains of a fourth-generation injection-use aminothiazole cephalosporins, which is cefpirome, and the quantity demanded in developing countries, such as China and India, is growing rapidly at present. The invention provides a production process of the 2,3- cyclopenteno pyridine. The specific process is as follows: (1) preparation of 4,5,6,7-tetrahydro-2-oxo-3-formyl cyclopenteno pyridine, (2) preparation of 2-chloro-2,3-cyclopenteno pyridine, and (3) preparation of the 2,3-cyclopenteno pyridine.
- -
-
-
- Modular Route to Azaindanes
-
A convergent radical based route to azaindanes is described, relying on the degenerative addition transfer of various substituted S-(pyridylmethyl)-O-ethyl dithiocarbonates (xanthates) to functional alkenes followed by radical cyclization onto the pyridine ring activated by protonation with trifluoroacetic acid. In one case, a richly decorated cyclohepta[b]pyridine could be assembled swiftly by allowing the first adduct to N-phenylmaleimide to undergo addition to N-allylphthalimide prior to cyclization.
- Huang, Qi,Zard, Samir Z.
-
supporting information
p. 3895 - 3898
(2017/07/26)
-
- Ligand-Enabled β-C–H Arylation of α-Amino Acids Without Installing Exogenous Directing Groups
-
Herein we report acid-directed β-C(sp3)-H arylation of α-amino acids enabled by pyridine-type ligands. This reaction does not require the installation of an exogenous directing group, is scalable, and enables the preparation of Fmoc-protected unnatural amino acids in three steps. The pyridine-type ligands are crucial for the development of this new C(sp3)-H arylation.
- Chen, Gang,Zhuang, Zhe,Li, Gen-Cheng,Saint-Denis, Tyler G.,Hsiao, Yi,Joe, Candice L.,Yu, Jin-Quan
-
p. 1506 - 1509
(2017/02/05)
-
- Design and synthesis of orally-active and selective azaindane 5HT2c agonist for the treatment of obesity
-
Based on our original pyrazine hit, CP-0809101, novel conformationally-restricted 5HT2c receptor agonists with 2-piperazin-azaindane scaffold were designed. Synthesis and structure-activity relationship (SAR) studies are described with emphasis on optimization of the selectivity against 5HT2a and 5HT2b receptors with excellent 2c potency. Orally-active and selective compounds were identified with dose-responsive in vivo efficacy in our pre-clinical food intake model.
- Liu, Kevin K.-C.,Cornelius, Peter,Patterson, Terrell A.,Zeng, Yuan,Santucci, Stephanie,Tomlinson, Elizabeth,Gibbons, Colleen,Maurer, Tristan S.,Marala, Ravi,Brown, Janice,Kong, Jimmy X.,Lee, Eunsun,Werner, Wendy,Wenzel, Zane,Vage, Chandra
-
scheme or table
p. 266 - 271
(2010/04/24)
-