36016-40-7Relevant articles and documents
Komplexchemie perhalogenierter Cyclopentadiene und Alkine. V. Darstellung weiterer funktioneller Derivate von (C5Cl4R)Mn(CO)3 und (C5Cl4R)Rh(COD). Kristallstruktur von (C5Cl4CONH2)Mn(CO)3
Suenkel, Karlheinz,Steiner, Doris
, p. 67 - 76 (1989)
Starting from (C5Cl4Li)Mn(CO)3, generated in situ, the functional derivatives (C5Cl4R)Mn(CO)3 with R = SnMe3, PPh2, SePh, (SCl5Cl4)Mn(CO)3, CHO, COCl, CONH2, CN, NCO, and NH2 can be obtained.A series of compounds (C5Cl4R)Rh(1,5-COD) with R = H, Me, SiMe3, SiMe2H and SnMe3 can be prepared from (C5Cl5)Rh(1,5-COD) via the lithio derivative.The crystal structure of (C5Cl4CONH2)Mn(CO)3 has been determined.
Synthesis of Pyrroles via Consecutive 6π-Electrocyclization/Ring-Contraction of Sulfilimines
Feichtinger, Niklas J.,Haut, Franz-Lucas,Müller, Mira,Magauer, Thomas,Plangger, Immanuel,Podewitz, Maren,Streit, Tim-Niclas,Wein, Lukas A.,Wurst, Klaus
supporting information, p. 9002 - 9008 (2021/07/01)
We present a modular, synthetic entry to polysubstituted pyrroles employing readily available 2,5-dihydrothiophenes. Ring-opening of the heterocycle provides access to a panel of 1,3-dienes which undergo pyrrole formation in the presence of inexpensive chloramine-T trihydrate. The transformation is conducted in an open flask and proceeds at ambient temperatures (23 °C) in nondry solvents. A careful adjustment of the electronics and sterics of the 1,3-diene precursor allows for the isolation of key intermediates. DFT studies identified a reaction mechanism that features a 6π-electrocyclization of a sulfilimine intermediate followed by spontaneous ring-contraction to reveal the pyrrole skeleton.
HYDROPYRAZINO[1,2-D][1,4]DIAZEPINE COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE
-
Page/Page column 21-22, (2021/05/07)
The present invention relates to compounds of formula (I), wherein R1 to R3 and n are as described herein, and their pharmaceutically acceptable salt thereof, and compositions including the compounds and methods of using the compounds.
Changing for the Better: Discovery of the Highly Potent and Selective CDK9 Inhibitor VIP152 Suitable for Once Weekly Intravenous Dosing for the Treatment of Cancer
Lücking, Ulrich,Kosemund, Dirk,B?hnke, Niels,Lienau, Philip,Siemeister, Gerhard,Denner, Karsten,Bohlmann, Rolf,Briem, Hans,Terebesi, Ildiko,B?mer, Ulf,Sch?fer, Martina,Ince, Stuart,Mumberg, Dominik,Scholz, Arne,Izumi, Raquel,Hwang, Stuart,Von Nussbaum, Franz
, p. 11651 - 11674 (2021/07/31)
Selective inhibition of exclusively transcription-regulating positive transcription elongation factor b/CDK9 is a promising new approach in cancer therapy. Starting from atuveciclib, the first selective CDK9 inhibitor to enter clinical development, lead optimization efforts aimed at identifying intravenously (iv) applicable CDK9 inhibitors with an improved therapeutic index led to the discovery of the highly potent and selective clinical candidate VIP152. The evaluation of various scaffold hops was instrumental in the identification of VIP152, which is characterized by the underexplored benzyl sulfoximine group. VIP152 exhibited the best preclinical overall profile in vitro and in vivo, including high efficacy and good tolerability in xenograft models in mice and rats upon once weekly iv administration. VIP152 has entered clinical trials for the treatment of cancer with promising longterm, durable monotherapy activity in double-hit diffuse large B-cell lymphoma patients.