77287-11-7Relevant articles and documents
Highly Diastereoselective Cycloadditions via Chelation Control: Asymmetric Synthesis of β-Lactones
Zemribo, Ronald,Romo, Daniel
, p. 4159 - 4162 (1995)
Chelation controlled cycloadditions of trimethylsilylketene to chiral α- and β-benzyloxyaldehydes followed by desilylation provides a highly diastereoselective route to functionalized β-lactones.Several Lewis acids were examined and MgBr2*Et2O was found to give the highest diastereoselectivities and yields.
COMPOUNDS FOR USE IN THE TREATMENT OR PROPHYLAXIS OF PAIN, INFLAMMATION AND/OR AUTOIMMUNITY
-
Page/Page column 15, (2020/08/13)
The present invention relates to a polymorphic form of (S,S)-2-N(3-O-(propan-2-ol)-1-propyl- 4-hydroxybenzene)-3-phenylpropylamide or synonymously named N-[2-(4-Hydroxy-phenyl)- -(2-hydroxy-propoxymethyl)-ethyl]-3-phenyl-propionamide and to the treatment
BENZAMIDE COMPOUNDS AS ROR GAMMA MODULATORS
-
Page/Page column 41, (2017/12/16)
The present disclosure is directed to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4, R5, n and p are as defined herein, which are active as modulators of retinoid-related orphan receptor gamma t (RORγt). These compounds prevent, inhibit, or suppress the action of RORγt and are therefore useful in the treatment of RORγt mediated diseases, disorders, syndromes or conditions such as, e.g., pain, inflammation, COPD, asthma, rheumatoid arthritis, colitis, multiple sclerosis, psoriasis, neurodegenerative diseases and cancer.
2 - (1 - hydroxyethyl), 2 - acetyl thiazole - 4 - carboxamides and application (by machine translation)
-
Paragraph 0013; 0020; 0021, (2017/11/16)
The invention relates to a 2 - (1 - hydroxyethyl), 2 - acetyl thiazole - 4 - carboxamides and application. This kind of structure of the compound of the general formula (I). Wherein X is OH (BB series), =O (BA series); R2 Is C2 - C5 alkyl, subs
Total synthesis and biological activity of dolastatin 16
Casalme, Loida O.,Yamauchi, Arisa,Sato, Akinori,Petitbois, Julie G.,Nogata, Yasuyuki,Yoshimura, Erina,Okino, Tatsufumi,Umezawa, Taiki,Matsuda, Fuyuhiko
supporting information, p. 1140 - 1150 (2017/02/10)
The total synthesis of dolastatin 16, a macrocyclic depsipeptide first isolated from the sea hare Dolabella auricularia as a potential antineoplastic metabolite by Pettit et al., was achieved in a convergent manner. Dolastatin 16 was reported by Tan to ex
Acyclic 1,4-Stereocontrol via the Allylic Diazene Rearrangement: Development, Applications, and the Essential Role of Kinetic e Stereoselectivity in Tosylhydrazone Formation
Shrestha, Maha L.,Qi, Wei,McIntosh, Matthias C.
, p. 8359 - 8370 (2017/08/23)
We report full details of a method for 1,3-reductive transposition of α-alkoxy-α,β-unsaturated hydrazones to provide E-alkenes with high 1,4-stereocontrol between the two respective allylic stereocenters. The process couples a chelation-controlled reduction of the hydrazone with an in situ allylic strain controlled retro-ene reaction of an allyl diazene, i.e., an allylic diazene rearrangement. Such stereotriads are frequently observed motifs in natural products. We observed a fortuitous kinetic preference for the E-hydrazone geometry during the hydrazonation reaction, as only the E-isomers could undergo chelation-controlled reduction.
Antineoplastic agents. 599. Total synthesis of dolastatin 16
Pettit, George R.,Smith, Thomas H.,Arce, Pablo M.,Flahive, Erik J.,Anderson, Collin R.,Chapuis, Jean-Charles,Xu, Jun-Ping,Groy, Thomas L.,Belcher, Paul E.,Macdonald, Christian B.
, p. 476 - 485 (2015/04/14)
The first 23-step total synthesis of the cyclodepsipeptide dolastatin 16 (1) has been achieved. Synthesis of the dolaphenvaline and dolamethylleuine amino acid units using simplified methods improved the overall efficiency. The formation of the 25-membere
Process for the Preparation of Triazole Antifungal Drug, Its Intermediates and Polymorphs Thereof
-
, (2014/12/09)
A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof. (I)
ISOLATED STEREOISOMERIC FORMS OF (S) 2-N (3-O-(PROPAN 2-OL) -1-PROPYL-4-HYDROXYBENZENE) -3-PHENYLPROPYLAMIDE
-
Page/Page column 15, (2013/06/27)
The present invention relates to isolated stereoisomeric forms of the compound (S)2-N(3- 0-(propan 2-ol)-l-propyl-4-hydroxybenzene)-3-phenylpropylamide. Specifically, the present invention relates to the use of (S)2-N(3-0-((S)propan 2-ol)-l-propyl-4- hydr
Total synthesis of incednam, the aglycon of incednine
Ohtani, Takashi,Tsukamoto, Shinya,Kanda, Hiroshi,Misawa, Kensuke,Urakawa, Yoshifumi,Fujimaki, Takahiro,Imoto, Masaya,Takahashi, Yoshikazu,Takahashi, Daisuke,Toshima, Kazunobu
scheme or table, p. 5068 - 5071 (2010/12/25)
The first total synthesis of incednam (1), the aglycon of antibiotic incednine (2), is described. Incednine has been reported to exhibit significant inhibitory activity against the antiapoptotic oncoproteins Bcl-2 and Bcl-xL. The synthesis of 1 commenced
