79099-07-3Relevant articles and documents
Synthesis of (R)-(+)-1,2,3,6-Tetrahydro-4-[U-14C]phenyl-1-[(3-phenyl-3-cyclohexenyl-1 -yl)methyl]pyridine, a potential antipsychotic agent
Ekhato,Huang
, p. 57 - 63 (1995)
1,2,3,6-Tetrahydro-4-[U-14C]phenylpyridine (12) was synthesized and coupled to (R)-3-phenyl-3-cyclohexene-1-carboxylic acid to make the titled compound 7 in 21% overall yield. Purification considerations were an important factor in the choice of a reaction sequence to 7, and successful synthesis was facilitated by the superiority of BF3.OEt2 as dehydrating reagent in this system. This otherwise problematic sequence offers an efficient and simple route to compound 7 (PD 143188).
ANTI-CD25 ANTIBODY-MAYTANSINE CONJUGATES AND METHODS OF USE THEREOF
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Paragraph 00402-00405, (2021/04/10)
The present disclosure provides anti-CD25 antibody-maytansine conjugate structures. The disclosure also encompasses methods of production of such conjugates, as well as methods of using the same.
A general N-alkylation platform via copper metallaphotoredox and silyl radical activation of alkyl halides
Cabré, Albert,Dow, Nathan W.,MacMillan, David W. C.
supporting information, p. 1827 - 1842 (2021/07/07)
The catalytic union of amides, sulfonamides, anilines, imines, or N-heterocycles with a broad spectrum of electronically and sterically diverse alkyl bromides has been achieved via a visible-light-induced metallaphotoredox platform. The use of a halogen abstraction-radical capture (HARC) mechanism allows for room temperature coupling of C(sp3)-bromides using simple Cu(II) salts, effectively bypassing the prohibitively high barriers typically associated with thermally induced SN2 or SN1 N-alkylation. This regio- and chemoselective protocol is compatible with >10 classes of medicinally relevant N-nucleophiles, including established pharmaceutical agents, in addition to structurally diverse primary, secondary, and tertiary alkyl bromides. Furthermore, the capacity of HARC methodologies to engage conventionally inert coupling partners is highlighted via the union of N-nucleophiles with cyclopropyl bromides and unactivated alkyl chlorides, substrates that are incompatible with nucleophilic substitution pathways. Preliminary mechanistic experiments validate the dual catalytic, open-shell nature of this platform, which enables reactivity previously unattainable in traditional halide-based N-alkylation systems.
FENTANYL HAPTENS FOR THE PREPARATION OF A FENTANYL VACCINE
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Paragraph 0195, (2021/07/24)
Described is the preparation of novel fentanyl haptens of Formula (1) through (6) and their use in the preparation of effective fentanyl vaccines.